- Crystalline and molecular structure of 2-amino-5-phenyl-1,3,4-thiadiazole
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The crystalline and molecular structure of 2-amino-5-phenyl-1,3,4-thiadiazole was studied by the X-ray diffraction method. C8H7N3S. Monoclinic crystals: a = 11.085 (3), b = 7.544 (3), c = 11. 180 (3) A; β = 115.22 (2)°; V
- Ishankhodzhaeva,Kadyrova,Surazhskaya,Parpiev,Koz'min
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- One pot synthesis and characterization of some novel Schiff bases with 1,3,4-thiadiazole unit
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A series of novel benzimidazole substituted Schiff bases were synthesized by the reaction of aromatic aldehydes with the corresponding ethyl acetoacetate or methyl acetoacetate and 1,3,4-thiadiazole. These compounds have been characterized by 1
- Zhao, Mengjie,Li, Xiao,Shang, Chengxiang,Zhang, Jian
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- An efficient synthesis of novel spiro[indole-3,8′-pyrano[2,3-d][1,3,4]thiadiazolo[3,2-a]pyrimidine derivatives via organobase-catalyzed three-component reaction of malononitrile, isatin and heterocyclic-1,3-diones
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In this research, firstly, some derivatives of sulfur containing [1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one have been synthesized and then they were used for the synthesis of novel derivatives of 6′-amino-2,9′-dioxo-2′-phenyl-9′H-spiro[indoline-3,8′-pyrano[2,3-d][1,3,4]thiadiazolo[3,2-a]pyrimidine]-7′-carbonitriles via a one-pot three-component condensation reaction of 7-hydroxy-2-phenyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one derivatives, malononitrile and isatin compounds in the presence of DABCO as a organocatalyst and under solvent-free conditions. In this report, a new family of spiro-pyrano-thiadiazolo-pyrimidine derivatives have been synthesized in short reaction times (10–60 min) and good to excellent yields (80–96%). The structures of all synthesized products have been confirmed by IR, 1H NMR, 13C NMR and mass spectrometry, and the structure of one selected product was characterized by single-crystal X-ray diffraction studies as well.
- Hosseini, Saedehsadat,Esmaeili, Abbas Ali,Khojastehnezhad, Amir,Notash, Behrouz
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- Design, synthesis and pharmacological evaluation of carboxamide and carbothioamide derivatives of 1,3,4-thiadiazole as the inhibitors of acetylcholinesterase and oxipiperazine)ative stress for the management of cognitive debility
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Acetylcholinesterase has been a promising target for the development of putative therapeutics against cognitive decline. The deleterious effect of oxidative stress on the learning and memory paradigms of an individual has also been well documented. In vie
- Kulshreshtha, Akanksha,Piplani, Poonam
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- Non-typical fluorescence effects and biological activity in selected 1,3,4-thiadiazole derivatives: Spectroscopic and theoretical studies on substituent, molecular aggregation, and pH effects
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The below article presents the results of spectroscopic research, theoretical (timedependent density functional theory (TD-DFT)), microbiological, and antioxidative calculations for three compounds from the group of 1,3,4-thiadiazoles: 2-amino-5-phenyl-1,
- Budziak, Iwona,Karc, Dariusz,Makowski, Marcin,Rachwa?, Kamila,Starzak, Karolina,Matwijczuk, Alicja,My?liwa-Kurdziel, Beata,Oniszczuk, Anna,Combrzyński, Maciej,Podle?na, Anna,Matwijczuk, Arkadiusz
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- Synthesis, Characterization and Biological Evaluation of Some Novel Azo-Imine Compounds
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The oxidative cyclization of thiosemicarbazone (III) synthesized from reaction between substituted aryl aldehydes (I) with thiosemicarbazide (II) was done using ferric chloride as oxidative agent to get 2-amino-5-phenyl-1,3,4-thiadiazole (IV). 2-Amino-5-phenyl-1,3,4-thiadiazole was introduced in condensation reactions with substituted aldehydes to obtain benzylidene imine derivatives (VI)1-5. Further these were treated with sulphanilic acid to give new 2-{[5-phenyl-1,3,4-thiadiazole-2-imino] substituted benzene}diazenyl benzene sulfonic acid derivatives (VII)1-5. These derivatives were further characterized by FT-IR, 1H NMR and 13C NMR spectral studies and were screened for antibacterial, antifungal and antioxidant activities.
- Nair, Smitha,Palanisamy, P.,Sunitha, K.
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p. 663 - 667
(2022/02/22)
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- Synthesis and preliminary anticancer activity assessment of n-glycosides of 2-amino-1,3,4-thiadiazoles
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The addition of 2-amino-1,3,4-thiadiazole derivatives with parallel iodination of differ-ently protected glycals has been achieved using a double molar excess of molecular iodine under mild conditions. The corresponding thiadiazole derivatives of N-glycosides were obtained in good yields and anomeric selectivity. The usage of iodine as a catalyst makes this method easy, inexpen-sive, and successfully useable in reactions with sugars. Thiadiazole derivatives were tested in a panel of three tumor cell lines, MCF-7, HCT116, and HeLa. These compounds initiated biological response in investigated tumor models in a different rate. The MCF-7 is resistant to the tested com-pounds, and the cytometry assay indicated low increase in cell numbers in the sub-G1 phase. The most sensitive are HCT-116 and HeLa cells. The thiadiazole derivatives have a pro-apoptotic effect on HCT-116 cells. In the case of the HeLa cells, an increase in the number of cells in the sub-G1-phase and the induction of apoptosis was observed.
- ?urawska, Katarzyna,Kapica, Patryk,Kasprzycka, Anna,Kudelko, Agnieszka,Olesiejuk, Monika,Papaj, Katarzyna,Skonieczna, Magdalena,Stokowy, Marcin,Szeja, Wies?aw,Walczak, Krzysztof
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supporting information
(2021/12/02)
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- Diversity-Oriented Synthesis of 1,2,4-Triazols, 1,3,4-Thiadiazols, and 1,3,4-Selenadiazoles from N-Tosylhydrazones
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The diversity-oriented synthesis of 1,2,4-triazols, 1,3,4-thiadiazols, and 1,3,4-selenadiazoles from N-tosylhydrazones was developed, and the reactions were general for a wide range of substrates, in which NH2CN, KOCN, KSCN, and KSeCN were used as odorless sources. Two different pathways were proposed, and N-tosylhydrazonoyl chlorides were formed in situ in the presence of NCS.
- Wei, Zeyang,Zhang, Qi,Tang, Meng,Zhang, Siyu,Zhang, Qian
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p. 4436 - 4440
(2021/05/26)
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- Synthesis of Emodin Amide Derivatives Containing 1,3,4-Thiadiazole and Their Inhibitory Activity on Vibrio harveyi
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A series of new 1,3,4-thiadiazole Emodin amide derivatives were synthesized through the connection of 5-substituted-1,3,4-thiadiazole-2-amine and Emodin carboxylic acids which were obtained by a two-step procedure starting from Emodin. Vibrio harveyi inhibition activities of the newly prepared compounds were evaluated. Results revealed that all compounds showed different degrees of inhibition on V. harveyi. Among them, compound 7a showed the best V. harveyi inhibition effect and the minimum inhibitory concentration (MIC) was 0.0625 mg/mL.
- Cao, Lian-Gong,Cao, Zhi-Ling,Chen, Chao,Jiang, Kai-Jun,Liu, Shu-Hao,Liu, Wei-Wei,Ruan, Xin-Chi,Shao, Zhong-Bai,Shi, Da-Hua,Su, Zi-Qin,Wang, You-Xian,Wu, Yu-Ran,Wu, Yu-Yu
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p. 281 - 286
(2021/08/05)
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- A novel approach to the synthesis of 1,3,4-thiadiazole-2-amine derivatives
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The main purpose of the study was the development of a new method for synthesis of 1,3,4-thiadiazol-2-amine derivatives in a one-pot manner using the reaction between a thiosemicarbazide and carboxylic acid without toxic additives such as POCl3 or SOCl2. The reaction was investigated in the presence of polyphosphate ester (PPE). It was found that, in the presence of PPE, the reaction between the thiosemicarbazide and carboxylic acid proceeds in one-pot through three steps with the formation of corresponding 2-amino-1,3,4-thiadiazole. Using the developed approach five, 2-amino-1,3,4-thiadiazoles were synthesized. The structures of all compounds were proven by mass spectrometry, IR, and NMR spectroscopies.
- Gadomsky, Svyatoslav Y.,Kokovina, Tatiana S.,Sanina, Nataliya A.,Terentiev, Alexei A.
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- COMPOUNDS HAVING PDE9A INHIBITORY ACTIVITY, AND PHARMACEUTICAL USES THEREOF
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The present invention provides a compound having a specific chemical structure and having PDE9A inhibitory activity, or a pharmaceutically acceptable salt thereof. The present invention provides a composition containing the compound or a pharmaceutically acceptable salt thereof. The present invention provides a pharmaceutical use, for treating or preventing PDE9A-related diseases, of the compound according to the present invention, a salt thereof, and a composition containing the compound or salt. The present invention also provides a method for treating or preventing PDE9A-related diseases, the method comprising administering an effective amount of the compound according to the present invention, a salt thereof, or a composition containing the compound or salt to a subject in need of treatment.
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Paragraph 0296-0300
(2021/10/15)
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- Gramine-based structure optimization to enhance anti-gastric cancer activity
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Gramine is a natural indole alkaloid with a wide range of biological activities, but its anti-gastric cancer activity is poor. Herein, a pharmacophore fusion strategy was adopted to design and synthesize a new series of indole-azole hybrids on the structural basis of gramine. Based on our previous studies, different nitrogen-containing five-membered heterocyclic rings and terminal alkyne group were introduced into the indole-based scaffold to investigate their effect on improving the anti-gastric cancer activity of gramine derivatives. Structure-activity relationship (SAR) studies highlighted the role played by terminal alkyne in enhancing the inhibitory effect, and compound 16h displayed the best antiproliferative activity against gastric cancer MGC803 cells with IC50 value of 3.74 μM. Further investigations displayed compound 16h could induce mitochondria-mediated apoptosis, and caused cell cycle arrest at G2/M phase. Besides, compound 16h could inhibit the metastasis ability of MGC803 cells. Our studies may provide a new strategy for structural optimization of gramine to enhance anti-gastric cancer activity, and provide a potential candidate for the treatment of gastric cancer.
- Zhang, Xin-Hui,Guo, Qian,Wang, Heng-Ying,Li, Yi-Han,Khamis, Mussa Yussuf,Ma, Li-Ying,Wang, Bo,Liu, Hong-Min
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- Synthesis and Biological Evaluation of Oxadiazole Clubbed Thiadiazole Derivatives as Antimicrobial Agents
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A series of 1,3,4-oxadiazole clubbed 1,3,4-thiadiazole derivatives were synthesized and assessed in vitro for their activity as antimicrobial agents. The target compounds 2-(5-(substituted aryl)-1, 3, 4-oxadiazol-2-ylthio)-N-(5-(substituted aryl)-1, 3, 4-thiadiazol-2-yl) acetamides (5a-5s) were synthesized using a basic condensation reaction between 5-(substituted aryl)-1,3,4-oxadiazole-2-thiol and 2-chloro-N-(5-(substituted aryl)-1,3,4-thiadiazol-2-yl)acetamide in presence of K2CO3 as a scavenging agent and acetone as reaction solvent. The titled compounds synthesized here, exhibited excellent to moderate antimicrobial activity against a broad panel of antibacterial strains of Gram-positive and Gram-negative bacteria and fungi.
- Begari, Eeshwaraiah,Dave, Alpa Y.,Joshi, Deepkumar S.,Parmar, Kokila A.
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p. 273 - 280
(2021/08/03)
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- Synthesis and antimicrobial activities of thiadiazole containing quinoline derivatives
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A novel series of 1-[(substituted 2-chloroquinolin-3-yl)methylidene]-3-[substituted-5-phenyl-1,3,4-thiadiazol-2-yl] thioureas have been synthesized by acid catalyzed reaction between the 1-(5-substitued phenyl-1,3,4-thiadiazol-2-yl) thioureas and 6-substi
- D'Souza, Vineetha Telma,Dayananda, P.,Nayak, Janardhana
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p. 633 - 638
(2021/09/28)
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- N-(5-phenyl-1, 3, 4-thiadiazole-2-yl) benzamide compound
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The invention belongs to the technical field of medicines, relates to a compound with antitumor activity and a specific chemical structure, and in particular relates to an N-((6, 7-dimethoxyquinoline-4-yl) oxy) methyl)-N-(5-phenyl-1, 3, 4-thiadiazole-2-yl) benzamide compound and a preparation method and an application thereof. The structural general formula of the compound is shown in the specification, wherein an R group is mono-substituted or double-substituted phenyl, fluorophenyl, chlorphenyl, bromophenyl, benzyl, benzyloxy, benzene nitro or trifluoromethyl substituted at 2-position, 3-position or 4-position. Pharmacological studies show that the compound provided by the invention has a relatively remarkable proliferation inhibition effect on HER-2 positive breast cancer cells SK-Br-3, the effect is obviously superior to that of HER-2 negative breast cancer cells MCF-7, the compound can be used for preparing antitumor drugs, and a new way is opened up for deep research and development of tumor drugs in the future. The preparation method provided by the invention is simple and feasible, relatively high in yield and easy for large-scale production.
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Paragraph 0051; 0057
(2021/06/09)
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- Aryl or heteroaryl substituted thiadiazole compound and antibacterial application thereof
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The invention belongs to the technical field of medicines, and particularly relates to an aryl or heteroaryl substituted thiadiazole compound, a preparation method and application thereof as an antibacterial drug. The compound is represented by formula (1
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Paragraph 0095-0097
(2021/01/30)
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- 1,3,4-Thiadiazole-Containing Azo Dyes: Synthesis, Spectroscopic Properties and Molecular Structure
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Three series of azo dyes derived from 2-amino-5-aryl-1,3,4-thiadiazoles and aniline, N,N-dimethylaniline and phenol were synthesized in high yields by a conventional diazotization-coupling sequence. The chemical structures of the prepared compounds were confirmed by 1H-NMR, 13C-NMR, IR, UV-Vis spectroscopy, mass spectrometry and elemental analysis. In addition, the X-ray single crystal structure of a representative azo dye was presented. For explicit determination of the influence of a substituent on radiation absorption in UV-Vis range, time-dependent density functional theory calculations were performed.
- Kudelko, Agnieszka,Olesiejuk, Monika,Luczynski, Marcin,Swiatkowski, Marcin,Sieranski, Tomasz,Kruszynski, Rafal
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- Design and development of 1,3,5-triazine-thiadiazole hybrids as potent adenosine A2A receptor (A2AR) antagonist for benefit in Parkinson's disease
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Various studies showed adenosine A2A receptors (A2ARs) antagonists have profound therapeutic efficacy in Parkinsons Disease (PD) by improving dopamine transmission, thus being active in reversing motor deficits and extrapyramidal symptoms related to the disease. Therefore, in the presents study, we have showed the development of novel 1,3,5-triazine-thiadiazole derivative as potent A2ARs antagonist. In the radioligand binding assay, these molecules showed excellent binding affinity with A2AR compared to A1R, with significant selectivity. Results suggest, compound 7e as most potent antagonist of A2AR among the tested series. In docking analysis with A2AR protein model, compound 7e found to be deeply buried into the cavity of receptor lined via making numerous interatomic contacts with His264, Tyr271, His278, Glu169, Ala63, Val84, Ile274, Met270, Phe169. Collectively, our study demonstrated 1,3,5-triazine-thiadiazole hybrid as a highly effective scaffold for the design of new A2A antagonists.
- Agnihotri, Amol Kumar,Bhat, Hans Raj,Giri, Sabeena,Masih, Anup,Pandey, Nidhi,Shrivastava, Jitendra Kumar,Singh, Saumya,Singh, Udaya Pratap
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- Synthesis and trypanocidal activity of novel pyridinyl-1,3,4-thiadiazole derivatives
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Herein, we present the design, synthesis and trypanocidal evaluation of sixteen new 1,3,4-thiadiazole derivatives from N-aminobenzyl or N-arylhydrazone series. All derivatives were assayed against the trypomastigote form of Trypanosoma cruzi, showing IC50 values ranging from 3 to 226 μM, and a better trypanocidal profile was demonstrated for the 1,3,4-thiadiazole-N-arylhydrazones (3a-g). In this series, the 2-pyridinyl fragment bound to the imine subunit of the hydrazine moiety presented pharmacophoric behavior for trypanocidal activity. Compounds 2a, 11a and 3e presented remarkable activity and excellent selectivity indexes. Compound 2a was also active against the intracellular amastigote form of T. cruzi. Moreover, its corresponding hydrochloride, compound 11a, showed the most promising profile, producing phenotypic changes similar to those caused by posaconazole, a well-known inhibitor of sterol biosynthesis. Thus, 1,3,4-thiadiazole derivative 11a could be considered a good prototype for the development of new drug candidates for Chagas disease therapy.
- Barbosa, Juliana M. C.,Bernardino, Patrícia,Decoté-Ricardo, Débora,Fraga, Carlos A. M.,Freitas, Rosana H. C. N.,Melo, Tatiana G.,Salom?o, Kelly,Sueth-Santiago, Vitor,Wardell, James L.,Wardell, Solange M. S. V.,da Silva, Edson F.
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- Synthesis, spectral characterization and DNA interactions of 5-(4-substituted phenyl)-1,3,4-thiadiazol-2-amine scaffolds
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Five 5-(4-Substituted phenyl)-1, 3, 4-thiadiazole-2-amines have been prepared and structure of the compounds confirmed by spectroscopy studies. On the basis of spectroscopic studies, confirmed the formation of compounds. The DNA binding affinity of the prepared compounds was undertaken by absorption titration method and increasing the amount of CT-DNA observed hyperchromism or hypsochromism. The binding affinity compounds (except 5) are in the order of 4[13.341 × 104 M?1]>3 [8.505 × 104 M-1]>2 [3.567 × 104 M-1]>1[3.525 × 104 M?1]. The ethidiumbromide quenching results indicates CT-DNA was quenched by thiadiazoles via a static quenching mechanism. The DNA cleavage studies of the compounds were carried out in the presence and absence of H2O2 using gel electrophoresis experiment.
- Shivakumara,Murali Krishna
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- Combined experimental and theoretical studies on a phenyl thiadiazole-based novel turn-on fluorescent colorimetric Schiff base chemosensor for the selective and sensitive detection of Al3+
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Herein, we have presented a phenyl thiadiazole-based Schiff base receptor, 2-[(Z)-(5-phenyl-1,3,4-thiadiazol-2-ylimino)methyl]-6-methoxy-4-nitrophenol (L) for the first time for turn-on fluorescent, colourimetric detection of Al3+ ions. The chemosensor L displayed very quick responses, excellent selectivity and sensitivity towards Al3+ ions in methanol-Tris-HCl buffer medium (10 mM, pH 7.2, and 1?:?1 v/v) with colourimetric and fluorometric detection limit values of 1.43 × 10-7 M and 1.15 × 10-7 M, respectively. The binding stoichiometry was obtained as 2?:?1 from the Job plot analysis and ESI-MS spectra with the association constant value of 1.76 × 102 M-1/2. The experimental results have further been supported by thorough DFT and TD-DFT studies. The chemosensor L can be applied for the formation of binary logical devices, recovery of contaminated water samples and smartphone-based chemical analysis.
- Manna, Amit Kumar,Chowdhury, Shubhamoy,Patra, Goutam K.
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p. 10819 - 10832
(2020/08/21)
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- Method for preparing 2-amino-5-substituted-1,3,4-thiadiazole
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The invention relates to a method for preparing 2-amino-5-substituted-1,3,4-thiadiazole, The method comprises: adding choline chloride and urea into a reaction container according to a formula ratio,and stirring at 80 DEG C to obtain a colorless transparent solution, ie., a eutectic solvent DES; cooling to a room temperature, adding carboxylic acid and thiosemicarbazide according to a formula ratio, slowly heating, reacting at 80 DEG C, and carrying out TLC monitoring until the reaction is finished; cooling the reaction mixed liquid to a room temperature, adding ammonia water into the mixed liquid under ice bath cooling to adjust the pH value to 8-9, precipitating the solid, carrying out suction filtration, washing the filter cake with ice water, and drying to obtain the 2-amino-5-substituted-1,3,4-thiadiazole; and recovering the filtrate to obtain the eutectic solvent capable of being repeatedly used. According to the invention, the method has characteristics of simple operation, simple post-treatment, short reaction time, high efficiency, catalyst recycling, environmental protection, cost reducing and no requirement of organic solvents, and is a method for efficiently synthesizing 2-amino-5-substituted-1,3,4-thiadiazole.
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Paragraph 0052-0058
(2020/02/14)
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- Synthesis of indole-tethered [1,3,4]thiadiazolo and [1,3,4]oxadiazolo[3,2-a]pyrimidin-5-one hybrids as anti-pancreatic cancer agents
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New indole-tethered [1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one (8a-j) and [1,3,4]oxadiazolo[3,2-a]pyrimidin-5-one hybrids (9a-e) were synthesized using [4+2] cycloaddition reactions of functionalized 1,3-diazabuta-1,3-dienes with indole-ketenes. All molecul
- Gummidi, Lalitha,Kerru, Nagaraju,Awolade, Paul,Raza, Asif,Sharma, Arun K.,Singh, Parvesh
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- Novel fatty acid-thiadiazole derivatives as potential antimycobacterial agents
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The discovery of antibiotics around the middle twentieth century led to a decrease in the interest in antimycobacterial fatty acids. In order to re-establish the importance of naturally abundant fatty acid, a series of fatty acid-thiadiazole derivatives were designed and synthesized based on molecular hybridization approach. In vitro antimycobacterial potential was established by a screening of synthesized compounds against Mycobacterium tuberculosis H37Rv strain. Among them, compounds 5a, 5d, 5h, and 5j were the most active, with compound 5j exhibiting minimum inhibitory concentration of 2.34?μg/ml against M.tb H37Rv. Additionally, the compounds were docked to determine the probable binding interactions and understand the mechanism of action of most active molecules on enoyl-acyl carrier protein reductases (InhA), which is involved in the mycobacterium fatty acid biosynthetic pathway.
- Mali, Jaishree K.,Sutar, Yogesh B.,Pahelkar, Akshata R.,Verma, Preeti M.,Telvekar, Vikas N.
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p. 174 - 181
(2019/11/03)
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- Further insight into the dual COX-2 and 15-LOX anti-inflammatory activity of 1,3,4-thiadiazole-thiazolidinone hybrids: The contribution of the substituents at 5th positions is size dependent
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Herin we report the design, synthesis, full characterization and biological investigation of new 15-LOX/COX dual inhibitors based on 1,3-thiazolidin-4-one (15-lipoxygenase pharmacophore) and 1,3,4-thiadiazole (COX pharmacophore) scaffolds. This series of molecular modifications is an extension of a previously reported series to further explore the structural activity relationship. Compounds 3a, 4e, 4n, 4q, 7 and 8 capable of inhibiting 15-LOX at (2.74, 4.2, 3.41, 10.21, 3.71 and 3.36 μM, respectively) and COX-2 at (0.32, 0.28, 0.28, 0.1, 0.28 and 0.27 μM, respectively). The results revealed that binding to 15-LOX and COX is sensitive to the bulkiness of the substituents at the 5 positions. 15-LOX bind better with small substituents, while COXs bind better with bulky substituents. Compounds 3a, 4r and 4q showed comparable in vivo anti-inflammatory activity to the reference drug (celecoxib). The ulcer liability test showed no sign of ulceration which ensures the safe gastric profile. Docking study was performed to explore the possible mode of interaction of the new compounds with the active site of human 15-LOX and COX-2. This study discloses some structural features for binding to 15-LOX and COX, thus pave the way to design anti-inflammatory agents with balanced dual inhibition of these enzymes.
- Abdel-Moty, Samia G.,Abdu-Allah, Hajjaj H. M.,Omar, Yasser M.
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- Synthesis of (1,3,4-thiadiazol-2-yl)-acrylamide derivatives as potential antitumor agents against acute leukemia cells
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A lead compound with the (1,3,4-thiadiazol-2-yl)-acrylamide scaffold was discovered to have significant cytotoxicity on several tumor cell lines in an in-house cell-based screening. A total of 60 derivative compounds were then synthesized and tested in a CCK-8 cell viability assay. Some of them exhibited improved cytotoxic activities. The most potent compounds had IC50 values of 1–5 μM on two acute leukemia tumor cell lines, i.e. RS4;11 and HL-60. Flow cytometry analysis of several active compounds and detection of caspase activation indicated that they induced caspase-dependent apoptosis. It was also encouraging to observe that these compounds did not have obvious cytotoxicity on normal cells, i.e. IC50 > 50 μM on HEK-293T cells. Although the molecular targets of this class of compound are yet to be revealed, our current results suggest that this class of compound represents a new possibility for developing drug candidates against acute leukemia.
- An, Ran,Guo, Chun,Li, Qing,Li, Yan,Wang, Renxiao,Xu, Yaochun,Zhou, Mi
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supporting information
(2020/03/25)
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- N-thiadiazole-4-hydroxy-2-quinolone-3-carboxamides bearing heteroaromatic rings as novel antibacterial agents: Design, synthesis, biological evaluation and target identification
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Due to the occurrence of antibiotic resistance, bacterial infectious diseases have become a serious threat to public health. To overcome antibiotic resistance, novel antibiotics are urgently needed. N-thiadiazole-4-hydroxy-2-quinolone-3-carboxamides are a potential new class of antibacterial agents, as one of its derivatives was identified as an antibacterial agent against S. aureus. However, no potency-directed structural optimization has been performed. In this study, we designed and synthesized 37 derivatives, and evaluated their antibacterial activity against S. aureus ATCC29213, which led to the identification of ten potent antibacterial agents with minimum inhibitory concentration (MIC) values below 1 μg/mL. Next, we performed bacterial growth inhibition assays against a panel of drug-resistant clinical isolates, including methicillin-resistant S. aureus, and cytotoxicity assays with HepG2 and HUVEC cells. One of the tested compounds named 1-ethyl-4-hydroxy-2-oxo-N-(5-(thiazol-2-yl)-1,3,4-thiadiazol-2-yl)-1,2-dihydroquinoline-3-carboxamide (g37) showed 2 to 128-times improvement compared with vancomycin in term of antibacterial potency against the tested strains (MICs: 0.25–1 μg/mL vs. 1–64 μg/mL) and an optimal selective toxicity (HepG2/MRSA, 110.6 to 221.2; HUVEC/MRSA, 77.6–155.2). Further, comprehensive evaluation indicated that g37 did not induce resistance development of MRSA over 20 passages, and it has been confirmed as a bactericidal, metabolically stable, orally active antibacterial agent. More importantly, we have identified the S. aureus DNA gyrase B as its potential target and proposed a potential binding mode by molecular docking. Taken together, the present work reports the most potent derivative of this chemical series (g37) and uncovers its potential target, which lays a solid foundation for further lead optimization facilitated by the structure-based drug design technique.
- Xue, Wenjie,Li, Xueyao,Ma, Guixing,Zhang, Hongmin,Chen, Ya,Kirchmair, Johannes,Xia, Jie,Wu, Song
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- I2 Promoted Synthesis of 2-Aminothiadiazoles Employing KSCN as a Sulfur Source Under Metal-Free Conditions
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A new three-component strategy from aldehyde, p-toluenesulfonyl hydrazide and potassium thiocyanate for the synthesis of 2-aminothiadiazoles promoted by I2 under metal-free conditions has been described. Potassium thiocyanate was used as an odo
- Zhu, Fuyuan,Yan, Zhaohua,Ai, Chengmei,Wang, Yanmei,Lin, Sen
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supporting information
p. 6561 - 6565
(2019/10/22)
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- Novel synthesized SLC-0111 thiazole and thiadiazole analogues: Determination of their carbonic anhydrase inhibitory activity and molecular modeling studies
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In the presented work, we report the design and synthesis of novel SLC-0111 thiazole and thiadiazole analogues (11a–d, 12a–d, 16a–c and 17a–d). A bioisosteric replacement approach was adopted to replace the 4-fluorophenyl tail of SLC-0111 with thiazole and thiadiazole ones, which were thereafter extended with lipophilic un/substituted phenyl moieties. All the newly synthesized SLC-0111 analogues were evaluated in vitro for their inhibitory activity towards a panel of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1) isoforms (hCA I, II, IX and XII), using a stopped-flow CO2 hydrase assay. All the examined isoforms were inhibited by the primary sulfonamide derivatives (11a–d and 12a–d) in variable degrees with the following KI ranges: 162.6–7136 nM for hCA I, 9.0–833.6 nM for hCA II, 7.9–153.0 nM for hCA IX, and 9.4–94.0 nM for hCA XII. In particular, compounds 12b and 12d displayed 5.5-fold more potent inhibitory activity (KIs = 8.3 and 7.9 nM, respectively) than SLC-0111 (KI = 45 nM) towards hCA IX. Molecular docking study was carried out for 12d within the hCA IX (PDB 3IAI) active site, to justify its inhibitory activity.
- Abo-Ashour, Mahmoud F.,Eldehna, Wagdy M.,Nocentini, Alessio,Ibrahim, Hany S.,Bua, Silvia,Abdel-Aziz, Hatem A.,Abou-Seri, Sahar M.,Supuran, Claudiu T.
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p. 794 - 802
(2019/04/13)
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- Novel C7-substituted coumarins as selective monoamine oxidase inhibitors: Discovery, synthesis and theoretical simulation
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There is a continued need to develop new selective human monoamine oxidase (hMAO) inhibitors that could be beneficial for the treatment of neurological diseases. However, hMAOs are closely related with high sequence identity and structural similarity, which hinders the development of selective MAO inhibitors. “Three-Dimensional Biologically Relevant Spectrum (BRS-3D)” method developed by our group has demonstrated its effectiveness in subtype selectivity studies of receptor and enzyme ligands. Here, we report a series of novel C7-substituted coumarins, either synthesized or commercially purchased, which were identified as selective hMAO inhibitors. Most of the compounds demonstrated strong activities with IC50 values (half-inhibitory concentration) ranging from sub-micromolar to nanomolar. Compounds, FR1 and SP1, were identified as the most selective hMAO-A inhibitors, with IC50 values of 1.5 nM (selectivity index (SI) 50 of 18 nM and 15 nM (SI > 2.74 and SI > 2.82). Docking calculations and molecular dynamic simulations were performed to elucidate the selectivity preference and SAR profiles.
- Wang, Dong,Hong, Ren-Yuan,Guo, Mengyao,Liu, Yi,Chen, Nianhang,Li, Xun,Kong, De-Xin
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- Novel 1,3,4-thiadiazole conjugates derived from protocatechuic acid: Synthesis, antioxidant activity, and computational and electrochemical studies
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A series of 15 novel 1,3,4-thiadiazole amide derivatives containing a protocatechuic acid moiety were synthesized and structurally characterized. In addition, the corresponding imino (4) and amino (5) analogues of a phenyl-substituted 1,3,4-thiadiazole am
- Jakovljevi?, Katarina,Joksovi?, Milan D.,Botta, Bruno,Jovanovi?, Ljiljana S.,Avdovi?, Edina,Markovi?, Zoran,Mihailovi?, Vladimir,Andri?, Marijana,Trifunovi?, Sne?ana,Markovi?, Violeta
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p. 585 - 598
(2019/07/05)
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- Benzoxazole/benzothiazole-derived VEGFR-2 inhibitors: Design, synthesis, molecular docking, and anticancer evaluations
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A novel series of benzoxazole/benzothiazole derivatives 4a–c–11a–e were designed, synthesized, and evaluated for anticancer activity against HepG2, HCT-116, and MCF-7 cells. HCT-116 was the most sensitive cell line to the influence of the new derivatives. In particular, compound 4c was found to be the most potent derivative against HepG2, HCT-116, and MCF-7 cells, with IC50 values = 9.45 ± 0.8, 5.76 ± 0.4, and 7.36 ± 0.5 μM, respectively. Compounds 4b, 9f, and 9c showed the highest anticancer activities against HepG2 cells with IC50 values of 9.97 ± 0.8, 9.99 ± 0.8, and 11.02 ± 1.0 μM, respectively, HCT-116 cells with IC50 values of 6.99 ± 0.5, 7.44 ± 0.4, and 8.15 ± 0.8 μM, respectively, and MCF-7 cells with IC50 values of 7.89 ± 0.7, 8.24 ± 0.7, and 9.32 ± 0.7 μM, respectively, in comparison with sorafenib as reference drug with IC50 values of 9.18 ± 0.6, 5.47 ± 0.3, and 7.26 ± 0.3 μM, respectively. The most active compounds 4a–c, 9b,c,e,f,h, and 11c,e were further evaluated for their VEGFR-2 inhibition. Compounds 4c and 4b potently inhibited VEGFR-2 at IC50 values of 0.12 ± 0.01 and 0.13 ± 0.02 μM, respectively, which are nearly equipotent to the sorafenib IC50 value (0.10 ± 0.02 μM). Furthermore, molecular docking studies were performed for all synthesized compounds to assess their binding pattern and affinity toward the VEGFR-2 active site.
- El-Helby, Abdel-Ghany A.,Sakr, Helmy,Eissa, Ibrahim H.,Al-Karmalawy, Ahmed A.,El-Adl, Khaled
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- Silica catalyzed one pot synthesis of hybrid thiazolidin-4-one derivatives as anti-tubercular and anti-inflammatory agent by attenuating COX-2 pathway
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A novel series of a hybrid class of hybrid thiazolidin-4-one derivatives were designed and synthesized through one-pot catalytic synthesis. The reaction was catalyzed in the presence of silica-H2SO4(+6). The derivatives computational
- Pathak, Prateek,Shukla, Parjanya Kumar,Naumovich, Vladislav,Grishina, Maria,Potemkin, Vladimir,Verma, Amita
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p. 2725 - 2759
(2019/08/08)
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- Synthesis, molecular docking, antimicrobial evaluation, and DNA cleavage assay of new thiadiazole/oxadiazole ciprofloxacin derivatives
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Abstract: Herein we report the synthesis of new N-4-piperazinyl thiadiazole and oxadiazole ciprofloxacin derivatives and their antibacterial and antimycobacterial activities. Although thiadiazole ciprofloxacin derivatives compound showed broad spectrum antibacterial activity against all the tested strains either Gram-positive or Gram-negative organisms, the oxadiazole derivatives exhibited weaker antibacterial and antimycobacterial activities than thiadiazole derivatives against most of the tested strains compared with the reference ciprofloxacin. Moreover, the antimycobacterial screening revealed that compounds which containing thiadiazole scaffold potently inhibited Mycobacterium smegmatis at MIC of 1.56 and 3.13, respectively, and modestly inhibited the drug-resistant strains. DNA cleavage assay revealed that thiadiazole ciprofloxacin derivatives inhibited supercoil relaxation, albeit to a lesser extent than ciprofloxacin, and it also increased the amount of nicked substrate produced. Graphic abstract: [Figure not available: see fulltext.].
- Mohammed, Hamada H. H.,Abbas, Samar H.,Abdelhafez, El-Shimaa M. N.,Berger, James M.,Mitarai, Satoshi,Arai, Masayoshi,Abuo-Rahma, Gamal El-Din A. A.
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p. 1809 - 1824
(2019/11/05)
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- Synthesis, in vitro and in silico Anti-Proliferative Studies of Novel Piperiene-Oxadiazole and Thiadiazole Analogs
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Piperine is a component of pepper which has earlier been reported as anticancer active compound. This work is emphasized on the design and synthesis of new hybrid piperine analogs by coupling piperine with the amine group of oxadiazoles and thiadiazoles.
- Amperayani,Parimi
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p. 2301 - 2307
(2020/01/08)
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- Spiro-heterocyclics: A convenient synthesis and antimicrobial activity of 3-(5- substituted phenyl-l,3,4-thiadiazole-2-yl)-5,8-dithiaspiro[3,4]octan-2-ones and 1,4-dithia-6-azaspiro[4,4]-nonan-7-ones
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A new series of novel 3-(5-substituted phenyl-l,3,4-thiadiazole-2-yl)-5,8-dithiaspiro[3,4]octan-2-ones and l,4-dithia-6- - azaspiro[4,4]nonan-7-ones have been synthesized from a common intermediate, in good yields. These compounds have been screened for t
- Tiwari, Shailendra
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p. 1416 - 1420
(2019/05/22)
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- PhI-Catalyzed Intramolecular Oxidative Coupling Toward Synthesis of 2-Amino-1,3,4-Thiadizoles
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A highly efficient method for the synthesis of thiadiazole derivatives via intramolecular oxidative coupling of thiosemicarbazide, using the in situ generated hypervalent iodine(III) reagents is developed. The protocol can be carried out smoothly and provides a variety of thiadiazole derivatives in moderate to excellent yields. Graphical Abstract: A highly efficient method for the synthesis of thiadiazole derivatives via PhI-catalyzed intramolecular oxidative coupling of thiosemicarbazide has been developed.
- Han, Yingzhi,Sun, Yadong,Abdukader, Ablimit,Liu, Bifu,Wang, Duozhi
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p. 3486 - 3491
(2018/09/27)
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- A green ultrasound synthesis, characterization and their antibacterial evaluation of novel transition metal complex of 2-amino-5-aryl-1, 3, 4-thiadiazole
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In the present study a series of metal complex of [bis (2-amino-5-aryl-1,3,4-thiadiazole]2Cl (S1-S9) was synthesized by using ultrasound irradiation technique. The metal complex was synthesized by the reaction between ligand and appropriate metal salts (CuCl2. 2H2O, CoCl2. 6H2O, ZnCl2, MgCl2. 4H2O, NiCl2. 6H2O). The products were obtained in high yield and the reaction time was found to be shorter. The synthesized metal complexes were characterized by using UV-visible spectroscopy, FTIR,1H NMR and Mass spectroscopy. The synthesized compounds were investigated for antibacterial potential against gram positive bacteria (Bacillus subtilis, Staphylococcus aureus) and gram negative bacteria (Pseudomonas aeruginosa, Escherichia coli). Significant activity was observed for synthesized metal complexes S6 and S7 against B. subtilis and S. aureus.
- Kanwar, Satinder,Mehta, Dinesh K.,Das, Rina,Gupta, Girish K.
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p. 633 - 639
(2019/05/01)
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- Synthesis and antifungal activities of drimane-amide derivatives from sclareol
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Aim and Objective: Plant diseases are caused by fungal pathogens lead to severe economic losses in many agriculture crops. And the increasing resistance of many fungi to commonly used antifungal agents necessitates the discovery and development of new fungicides. So this study was focused on synthesizing novel skeleton compounds to effectively control plant diseases. Materials and Methods: A series of drimane-amide derivatives were designed, synthesized by aminolysis reaction of amine with intermediate sclareolide which was prepared from sclareol. The structures of all the synthesized compounds were confirmed using1H NMR,13C NMR, and HR-MS (ESI) spectroscopic data. Their in vitro antifungal activity were preliminarily evaluated by using the mycelium growth rate method against five phytopathogenic fungi: Botrytis cinerea, Glomerella cingulata, Alternaria alternate, Alternaria brassicae, and Fusarium graminearum. Results: 23 target compounds were successfully obtained in yields of 52-95%. Compounds358 A2 and A3 displayed favorable inhibitory potency against B. cinerea, G. cingulata and A. brassicae with IC50 values ranging from 3.18 to 10.48 μg/mL. These two compounds displayed higher fungicidal activity than sclareol against all the tested phytopathogenic fungi, and were more effective than the positive control thiabendazole against A. alternate and A. brassicae. The structure-activity relationship studies of compounds A1-10 indicated that both the position and type of substituent on the phenyl ring had significant effects on antifungal activity. Conclusion: The drimane-amide derivatives A2 and A3 were the most promising derivatives and should be selected as new templates for the potential antifungal agents.
- Ma, Miaofeng,Feng, Jili,Wang, Dezhi,Chen, Shu-Wei,Xu, Hui
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p. 501 - 509
(2018/12/13)
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- Preparation method and application of 1,3,4-thiadiazole (oxadiazole)-phenazine-1-formamide compound
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The invention discloses a 1,3,4-thiadiazole (oxadiazole)-phenazine-1-formamide compound. The structure of the compound is as shown in a formula (I), wherein R is at least one of hydrogen, halogen, nitryl, hydroxyl and alkyl or alkoxy of which the carbon a
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Paragraph 0045; 0046
(2018/04/26)
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- Novel fluorescent N,O-chelated fluorine-boron benzamide complexes containing thiadiazoles: Synthesis and fluorescence characteristics
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A series of N-(5-phenyl-1,3,4-thiadiazol-2-yl)benzamide derivatives and their corresponding BF2 complexes were synthesized, and their photophysical properties were determined. The effect of the derivatives with various substituents on the benza
- Zhang, Kan,Zheng, Hao,Hua, Chaojun,Xin, Ming,Gao, Jianrong,Li, Yujin
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supporting information
p. 4161 - 4167
(2018/07/06)
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- Design, Synthesis, and Biological Evaluation of Novel 1,3,4-Thiadiazolylpyrazolines Compounds Containing Ferrocene
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The synthesis of 1,3,4-thiadiazole skeleton compounds exhibiting high fungicidal activities has been demonstrated. Thirteen novel 1,3,4-thiadiazolyl-pyrazolines compounds containing ferrocene were designed and synthesized from the ferrocenylchalcones intermediates 3a–3m and the 2-hydrazino-5-phenyl-1,3,4-thiadiazole intermediate 8. All compounds were characterized by 1H NMR, 13C NMR, FT-IR spectra, and HR-MS, and the structure of one of the new compounds N-(4-phenyl-1,3,4-thiadiazol-2-yl)-3-ferrocenyl-5-phenyl-pyrazoline 9a was further determined by X-ray diffraction analysis. The preliminary results of a biological activity assay indicated that all the title compounds exhibited significant fungicidal activities against Pythium solani, Gibberella saubinetii, and Gibberella nicotiancola. Furthermore, compounds 9e and 9h displayed even higher fungicidal activities against the three fungal species compared with the control drug pyraclostrobin.
- Chen, Liqin,Duan, Huihui,Zhang, Xinyu,Zhang, Qiong,Huang, Hailian,Zhao, Junlong,Chen, Bang,Hua, Chengwen,Gou, Xiaofeng
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p. 1978 - 1985
(2018/07/31)
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- Synthesis and molecular simulation study of furoic peptidomimetic derivatives as potent aminopeptodase N inhibitors
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The aminopeptidase N (APN) plays a critical role in angiogenesis and is over-expressed in tumor cells. In this paper, we report the synthesis and enzyme inhibition assay of furoic peptidomimetic compounds. These new compounds exhibit potent inhibitory ability toward APN with IC50 values lying in the micromolar level. The binding mode of inhibitors in APN active site was explained by a molecular simulation study. These data reveal that ligand coordinating with the catalytic Zn-ion is very important for inhibitory activities.
- Gao, Min,He, Junhua,Xu, Weidong,Lai, Xiaoping,Liu, Fen,Tu, Guogang
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p. 123 - 127
(2018/03/25)
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- Synthesis of matrinic amide derivatives containing 1,3,4-thiadiazole scaffold as insecticidal/acaricidal agents
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In continuation of our program aimed at the development of natural product-based pesticidal agents, a series of matrinic amide derivatives containing 1,3,4-thiadiazole scaffold were prepared, and their insecticidal and acaricidal activities were evaluated against Mythimna separata and Tetranychus cinnabarinus. Some compounds exhibited potent insecticidal and acaricidal activities. It suggested that R1 as a nitro group and R2 as a fluorine atom, were important for the insecticidal activity; R1 as the electron-donating groups and R2 as the methyl group, were necessary for the acaricidal activity.
- Lv, Min,Liu, Guangci,Jia, Minghong,Xu, Hui
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- Heterocycles 48. synthesis, characterization and biological evaluation of imidazo[2,1-b][1,3,4]thiadiazole derivatives as anti-inflammatory agents
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Non-steroidal anti-inflammatory drugs (NSAIDs) are an important pharmacological class of drugs used for the treatment of inflammatory diseases. They are also characterized by severe side effects, such as gastrointestinal damage, increased cardiovascular r
- Cristina, Anamaria,Leonte, Denisa,Vlase, Laurian,Bencze, László Csaba,Imre, Silvia,Marc, Gabriel,Apan, Bogdan,Mogosan, Cristina,Zaharia, Valentin
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- Metal-free synthesis of 2-aminothiadiazoles via TBHP-Mediated oxidative C-S bond formation
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An efficient one-pot synthesis of 2-amino-1,3,4-thiadiazoles from easily available aldehydes and thiosemicarbazide using TBHP as an oxidant has been described. Notably, these reactions were carried out at room temperature using ethanol as solvent. This is the first example for one-pot synthesis of 2-amino-1,3,4-thiadiazole derivatives from aldehydes. This new synthetic methodology provides a simple procedure utilizing a safer oxidizing system that affords the target products in mild reaction condition with satisfactory yields and wide substrate scope.
- Hatvate, Navnath T.,Ghodse, Shrikant M.,Telvekar, Vikas N.
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supporting information
p. 285 - 290
(2018/02/09)
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- Design, synthesis and molecular docking of novel structural hybrids of substituted isatin based pyrazoline and thiadiazoline as antitumor agents
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Cancer, which is considered to be the world’s most serious illness cause 8.2 million deaths and this rate may double by 2030. We herein report a new series of 3-(2-(p-substituted)-2-((5-phenyl-1,3,4-thiadiazol-2-yl)imino)-2-(p-substituted)ethylidene)indolin-2-one (15–19) and 5-substituted-5′-substituted phenyl-2′,4′-dihydrospiro[indoline-3,3′-pyrazol]-2-one derivatives (20–24) as potent anticancer agents. These compounds were evaluated for in vitro antitumor activity against the National Cancer Institute panel of 60 cancer cell lines. Among all the synthesized compounds, two compounds 15 and 16 showed remarkable antitumor activity with GI50 (MG-MID) values of 0.65 & 0.72 μM, respectively against Non-small cell lung cancer. To gain insight for mode of binding with Epidermal Growth Factor Receptor kinase enzyme, these compounds were further subjected to docking studies.
- Gangarapu, Kiran,Thumma, Gouthami,Manda, Sarangapani,Jallapally, Anvesh,Jarapula, Ravi,Rekulapally, Sriram
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p. 819 - 829
(2017/03/06)
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- Cyclization–oxidation of Benzylidenehydrazinecarbothioamides by FeCl3.6H2O or ZnCl2.6H2O Catalysts and Synthesis of New 1,3,4-Thiadiazolo-[3,2- α]Pyrimidines
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We report new method for preparation of 2-amino-5-aryl-1,3,4-thiadiazoles by reaction of arylaldehyde with thiosemicarbazide and in the next step via cyclization of 2-aryl hydrazinecarbothioamide in the presence of ZnCl2.6H2O or FeCl3.6H2O. Also, in this research, new substituted 1,3,4-thiadiazolo-[3,2-α]pyrimidines were synthesized by the reaction of 2-amino-5-aryl-1,3,4-thiadiazoles derivatives with DMAD or DEAD in the presence of K2CO3 under reflux conditions. The FT-IR, 1H-NMR, 13C-NMR, elemental analysis and single- crystal X-ray analysis confirm the structures of the products.
- Darehkordi, Ali,Zarezadeh Abarqouei, Behnam,Rahmani, Fariba
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p. 1872 - 1879
(2017/05/29)
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- Phenyl substituted thiadiazole thiazolinone compound, preparation method and application thereof
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The invention discloses a phenyl substituted thiadiazole thiazolinone compound. A chemical construction thereof is shown as following formula. According to the invention, the phenyl substituted thiadiazole thiazolinone compound is prepared according the f
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Paragraph 0046; 0047; 0048; 0049; 0081; 0082; 0083-0085
(2018/04/01)
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- Synthesis and applications of pyridazinones for base oil improvement
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THREE pyridazinone derivatives of the type 4,5-dihydropyridazin- 3(2H)-ones, N-(4-(6-oxo-5- ((5-phenyl-1,3,4-thiadiazol-2-yl)amino) - 1,4,5,6 - tetrahydropyridazin - 3-yl) phenyl) acetamide (4a), 6-(4-chlorophenyl)-4-((5-phenyl-1,3,4-thiadiazol-2-yl)amino)-4,5-di-hydropyridazin-3 (2H)-one (4b) and 6-(4-bromophenyl) -4- ((5-phenyl-1,3,4-thiadiazol-2-yl) amino)-4,5-dihydropyridazin-3(2H)-one (4c) were synthesized. They were characterized by the conventional tools of analysis, Elemental analysis, IR and 1H-NMR spectroscopy. The tools of analysis confirmed the structure of the three prepared compounds. These heterocyclic compounds are chemically stable and possess multi actions for base oil improvement. They are tested as antioxidants for local base oil through the change in total acid number (TAN). They gave good results as antioxidants for base oil. Also these three synthesized compounds are tested as corrosion inhibitors for carbon steel in acid medium. The efficiency order for these tested compounds is ranked as follows: 4a > 4b > 4c. Energy of the highest occupied molecular orbital (EHOMO) and lowest unoccupied molecular orbital (ELUMO) for the three prepared compounds were calculated via the Ab initio method. Studying of the quantum chemical calculations of the synthesized compounds showed good matching with the experimental results.
- Rizk,Attia,Osman, Doaa I.,Nessim
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p. 129 - 146
(2017/06/13)
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- 2-phenyl-6-ferrocenyl-imidazo[2,1-b]-1,3,4-thiadiazole preparation method
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The present invention discloses a 2-phenyl-6-ferrocenyl-imidazo[2,1-b]-1,3,4-thiadiazole preparation method, which comprises: carrying out stirring mixing on 2-amino-5-phenyl-1,3,4-thiadiazole, alpha-bromo-acetylferrocene and ethanol; placing the mixed so
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Paragraph 0025; 0029; 0030; 0040; 0050; 0060; 0070
(2018/01/12)
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