- Synthesis of novel acylthioureas bearing naphthoquinone moiety as dual sensor for high-performance naked-eye colorimetric and fluorescence detection of CN? and F? ions and its application in water and food samples
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In this study, six new acylthiourea, bearing naphthoquinone moiety, sensors were synthesized in high yield (88–96%) and characterized using 1H/13C NMR, FT-IR and HRMS techniques. All synthesized sensors (4a-f) showed shifts in absorb
- ?ahin, Ertan,Ayd?ner, Burcu,Efeo?lu, ?a?la,Karasu, Elize,Kele?, Ergin,Nural, Yahya,Sefero?lu, Nurgül,Sefero?lu, Zeynel
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- Synthesis, characterization, antimicrobial, antioxidant and computational evaluation of N-acyl-morpholine-4-carbothioamides
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Abstract: The present research paper reports the convenient synthesis, successful characterization, in vitro antibacterial, antifungal, antioxidant potency and biocompatibility of N-acyl-morpholine-4-carbothioamides (5a–5j). The biocompatible derivatives were found to be highly active against the tested bacterial and fungal strains. Moreover, some of the screened N-acyl-morpholine-4-carbothioamides exhibited excellent antioxidant potential. Docking simulation provided additional information about possibilities of their inhibitory potential against RNA. It has been predicted by in silico investigation of the binding pattern that compounds 5a and 5j can serve as the potential surrogate for design of novel and potent antibacterial agents. The results for the in vitro bioassays were promising with the identification of compounds 5a and 5j as the lead and selective candidate for RNA inhibition. Results of the docking computations further ascertained the inhibitory potential of compound 5a. Based on the in silico studies, it can be suggested that compounds 5a and 5j can serve as a structural model for the design of antibacterial agents with better inhibitory potential. Graphic abstract: Binding mode of compound 5j inside the active site of RNA in 3D space. 5j displayed highest antibacterial potential than the reference drug ampicillin with ZOI 10.50?mm against Staphylococcus aureus. 5j also displayed highest antifungal potential than the reference drug amphotericin B with ZOI 18.20?mm against Fusarium solani.[Figure not available: see fulltext.].
- Aziz, Hamid,Saeed, Aamer,Khan, Muhammad Aslam,Afridi, Shakeeb,Jabeen, Farukh
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p. 763 - 776
(2020/03/04)
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- Analysis of the structural, spectroscopic, and molecular electrostatic potential (MESP) of (amino)carbonothionyl (nitro)benzamide derivatives
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This study examined the structural and spectroscopic properties of ten synthesized derivatives of carbonothionylbenzamide. These nitro group based molecules are five meta- (named M) and five para- (named P) compounds. These compounds showed no significant
- Fayomi, Omotola M.,Adeniyi, Adebayo A.,Sha’Ato
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p. 690 - 701
(2021/05/11)
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- Synthesis and antituberculosis activity of new acylthiosemicarbazides designed by structural modification
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Acylthiosemicarbazides 8a–n were designed by structural modification of lead Compound 7. The syntheses of 8a–n involve a five-step procedure starting from carboxylic acids. Compounds 8a–n were tested against three Mycobacterium tuberculosis strains to measure their inhibitory antituberculosis activities. These activities could be explained according to the presence or absence of the chlorine substituent in the aromatic ring of the amide joined to the thiosemicarbazide core. Thiosemicarbazide derivative 8n is a candidate for the development of novel antitubercular agents. Ongoing studies are focused on exploring the mechanism by which these compounds inhibit M. tuberculosis cell growth.
- Martínez, Roberto,Espitia-Pinzón, Clara I.,Silva Miranda, Mayra,Chávez-Santos, Rosa María,Pretelin-Castillo, Gustavo,Ramos-Orea, Aldahir,Hernández-Báez, ángela M.,Cotlame-Pérez, Sandra,Pedraza-Rodríguez, Rogelio
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p. 350 - 355
(2019/12/03)
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- Novel N-Acyl-1H-imidazole-1-carbothioamides: Design, Synthesis, Biological and Computational Studies
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The present study reports the convenient synthesis, spectroscopic characterization, bio-assays and computational evaluation of a novel series of N-acyl-1H-imidazole-1-carbothioamides. The screened derivatives displayed excellent antioxidant activity, moderate antibacterial and antifungal potential. The screened derivatives were found to be highly biocompatible against hRBCs. Molecular docking ascertained the mechanism and mode of action towards the molecular target delineating that ligands and complexes were stabilized at the active site by electrostatic and hydrophobic forces in accordance to the corresponding experimental results. Docking simulation provided additional information about the possibilities of inhibitory potential of the compounds against RNA. Computational evaluation predicted that N-acyl-1H-imidazole-1-carbothioamides 5c and 5g can serve as potential surrogates for hit to lead generation and design of novel antioxidant and antibacterial agents.
- Aziz, Hamid,Saeed, Aamer,Khan, Muhammad Aslam,Afridi, Shakeeb,Jabeen, Farukh,Ashfaq-ur-Rehman,Hashim, Muhammad
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- Benzoylthioureas: Design, synthesis and antimycobacterial evaluation
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Background: New drugs and strategies to treat tuberculosis (TB) are urgently needed. In this context, thiourea derivatives have a wide range of biological activities, including anti-TB. This fact can be illustrated with the structure of isoxyl, an old anti-TB drug, which has a thiourea as a pharmacophore group. Objective: The aim of this study is to describe the synthesis and the antimycobacterial activity of fifty-nine benzoylthioureas derivatives. Methods: Benzoylthiourea derivatives have been synthesized and evaluated for their activity against Mycobacterium tuberculosis using the MABA assay. After that, a structure-activity relationship study of this series of compounds has been performed. Results and Discussion: Nineteen compounds exhibited antimycobacterial activity between 423.1 and 9.6 μM. In general, we observed that the presence of bromine, chlorine and t-Bu group at the para-position in benzene ring plays an important role in the antitubercular activity of Series A. These substituents were fixed at this position in benzene ring and other groups such as Cl, Br, NO2 and OMe were introduced in the benzoyl ring, leading to the derivatives of Series B. In general, Series B was less cytotoxic than Series A, which indicates that the presence of a substituent at benzoyl ring contributes to an improvement in both antimycobacterial activity and toxicity profiles. Conclusion: Compound 4c could be considered a good prototype to be submitted to further structural modifications in the search for new anti-TB drugs, since it is 1.8 times more active than the first line anti-TB drug ethambutol and 0.65 times less active than isoxyl.
- Abreu, Lethícia O.,Bispo, Marcelle L. F.,Brito, Tiago O.,Gomes, Karen M.,Louren?o, Maria C. S.,Macedo, Fernando,Pereira, Patricia M. L.,Tisher, Cesar A.,Yamada-Ogatta, Sueli F.,de Fátima, ?ngelo
-
-
- Synthesis, characterization and biological activity of some dithiourea derivatives
-
Novel dithiourea derivatives have been designed as HIV-1 protease inhibitors using Autodock 4.2, synthesized and characterized by spectroscopic methods and microanalysis. 1-(3-Bromobenzoyl)-3-[2-({[(3-bromophenyl)formami-do]methanethioyl}amino)phenyl]thio
- Frost, Carminita,Hoppe, Heinrich,Hosten, Eric,Isaacs, Michelle,Khanye, Setshaba D.,Krause, Jason,Lobb, Kevin,Odame, Felix,Sayed, Yasien,Tshentu, Zenixole
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p. 764 - 777
(2020/10/02)
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- 4-aminocoumarin based aroylthioureas as potential jack bean urease inhibitors; synthesis, enzyme inhibitory kinetics and docking studies
-
Background: Urease enzyme catalyzes the hydrolysis of urea into ammonia and CO2, excess ammonia causes global warming and crop reduction. Ureases are also responsible for certain human diseases such as stomach cancer, peptic ulceration, pyelone
- Abbas, Qamar,Ashraf, Zaman,Channar, Pervaiz A.,Fattah, Tanzeela A.,Hassan, Mubashir,Larik, Fayaz A.,Saeed, Aamer
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p. 229 - 243
(2020/03/06)
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- Phosphine-free direct conversion of carboxylic acids into acyl isothiocyanates using various electrophilic halogenation reagents
-
In this study, the efficiency of some electrophilic halogen reagents including 2,4,6-trichloro-1,3,5-triazine, 2,4,4,6-tetrabromo-2,5-cyclohexadienone, 2-chloro-1-methylpyridinium iodide, N-bromosuccinimide, trichloroisocyanuric acid, and 1,3-dibromo-5,5-
- Khaje-Kolaki, Aslan,Mokhtari, Babak
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p. 805 - 808
(2018/09/26)
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- Synthesis, carbonic anhydrase inhibitory activity and antioxidant activity of some 1,3-oxazine derivatives
-
(Table presented.). A series of 1-(6-methyl-2-substituted phenyl-4-thioxo-4H-1,3-oxazin-5-yl)ethanones (3a-n) were synthesized by the reaction of benzoyl isothiocyanates with active methylene compound acetylacetone in the presence of triethyl amine in a one-pot process. The structures of the products were elucidated by elemental analyses, FT-IR, 1H NMR, 13C NMR, and mass spectroscopy. These new 1,3-oxazine derivatives were evaluated for their inhibitory activity against carbonic anhydrase II. Results for in vitro assay revealed that compound 3b having 4-methoxy phenyl moiety was the most potent inhibitor with IC50 value of 0.144 ± 0.008 μM. It exhibited higher enzyme inhibitory activity as compared to the standard acetazolamide (IC50 = 0.997 ± 0.061 μM). The compounds 3c, 3h, and 3n also displayed superior inhibitory activities compared to the rest of the synthesized oxazine derivatives. The radical scavenging activity of oxazine derivatives was also performed and it was found that compounds showed moderate antioxidant activity. Lipinski rule confirmed the therapeutic potential of the synthesized compounds. Molecular docking studies were also performed to further understand the binding affinity of these compounds with PDBID 1V9E which confirmed that the synthesized derivatives bind in the active binding site of the target protein. Based upon our results, it is proposed that compound 3b may serve as a lead structure to design more potent carbonic anhydrase inhibitors.
- Qamar, Rabia,Saeed, Aamer,Saeed, Maria,Ashraf, Zaman,Abbas, Qamar,Hassan, Mubashir,Albericio, Fernando
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p. 352 - 361
(2018/10/20)
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- Synthesis and antitumor activity of novel N-benzoyl-N'-substituted pyrimidinyl (thio)semicarbazide derivatives
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A series of substituted pyrimidinyl (thio)semicarbazide derivatives were designed and synthesized. The antitumor results showed that the activity of thiosemicarbazide compounds (series II) was generally higher than that of the corresponding semicarbazide derivatives (series I). Among them, IIk displayed higher cytotoxicity against HL-60, BGC-823 and Bel-7402 than that of adriamycin and exhibited broad in vitro cytotoxicity against 13 human tumor cell lines. Meanwhile, the cytotoxic selectivity and anti-multidrug resistance were evaluated, and IIk exhibited selective cytotoxicity against cancer cells in comparison to human normal cells and had significant anti-multidrug resistance capability. The bioassay results showed that IIk showed great promise as a potent lead compound for further antitumor discovery.
- Song, Gaopeng,Li, Jianzuo,Tian, Hao,Li, Yasheng,Hu, Dekun,Li, Ying,Cui, Zining
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p. 329 - 334
(2016/04/04)
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- Identification of acylthiourea derivatives as potent Plk1 PBD inhibitors
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Thiourea derivatives have drawn much attention for their latent capacities of biological activities. In this study, we designed acylthiourea compounds as polo-like kinase 1 (Plk1) polo-box domain (PBD) inhibitors. A series of acylthiourea derivatives without pan assay interference structure (PAINS) were synthesized. Four compounds with halogen substituents exhibited binding affinities to Plk1 PBD in low micromole range. The most potent compound (3v) showed selectivity over other subtypes of Plk PBDs and inhibited the kinase activity of full-length Plk1.
- Yun, Taikangxiang,Qin, Tan,Liu, Ying,Lai, Luhua
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p. 229 - 236
(2016/09/09)
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- Design, syntheses and evaluation of benzoylthioureas as urease inhibitors of agricultural interest
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Urea is one of the most used nitrogen fertilizers worldwide. However, occurrence of urea hydrolysis to ammonia and carbon dioxide on soil surface, catalyzed by soil ureases, considerably reduces nitrogen availability to crops. In this study, we describe the design, synthesis and screening of sixty five benzoylthioureas (BTUs) for their ability to inhibit purified jack bean and soil ureases. BTUs were readily obtained in one pot, two steps synthesis with no need of cumbersome procedures for product purification. In vitro assays revealed BTUs 11, 12, 14, 19-22 and 37 as the most active jack bean urease inhibitors. Such BTUs were found to be able to bind to both catalytic and allosteric sites of urease, acting therefore as mixed-type inhibitors. Out of 28 compounds that effectively inhibited soil ureases activity, BTUs 3, 6, 10, 12, 16, 19 and 22 were determined to be more potent than the reference inhibitor N-(butyl) thiophosphoric triamide (NBPT; 40%). The other 22 BTUs were as potent as NBPT on soil ureases. The temperature-tolerance of BTUs, along with their ability to inhibit soil ureases, makes of this class of compounds potential additive for urea-based fertilizers.
- Brito, Tiago O.,Souza, Aline X.,Mota, Yane C. C.,Morais, Vinicius S. S.,De Souza, Leandro T.,De Fátima, ?ngelo,Macedo, Fernando,Modolo, Luzia V.
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p. 44507 - 44515
(2015/06/02)
-
- Straightforward Approach Toward Dihydrothiazoles via Intramolecular Bromocyclization
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An intramolecular bromonium ion-assisted cyclization with sulfur as an internal nucleophile is described. Starting from benzoyl chlorides, this method provides an easy procedure for the synthesis of dihydrothiazole derivatives in moderate to good yields.
- Sadat-Ebrahimi, Seyed Esmail,Ganjizadeh Zarj, Marzieh,Moghimi, Setareh,Yahya-Meymandi, Azadeh,Mahdavi, Mohammad,Arab, Saman,Shafiee, Abbas,Foroumadi, Alireza
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p. 2142 - 2147
(2015/09/01)
-
- Synthesis of 2-aryl-7-methyl-4-thioxo-4H-pyrano[3,4-e][1,3]oxazin-5-one by three-component condensation
-
A novel method for oxazine ring formation is established though the reaction of ammonium thiocyanate and aroyl chlorides with 4-hydroxy-6-methyl-2H-pyran-2-one in the presence of N-methylimidazole to afford 2-aryl-7-methyl-4-thioxo-4H-pyrano[3,4-e][1,3]ox
- Khazaeian, Ali,Hassanabadi, Alireza
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p. 492 - 493
(2015/11/03)
-
- Direct and facile synthesis of acyl isothiocyanates from carboxylic acids using trichloroisocyanuric acid/triphenylphosphine system
-
A mild, efficient, and practical method for one-step synthesis of alkanoyl and aroyl isothiocyanates from carboxylic acids using a safe and inexpensive mixed reagent, trichloroisocyanuric acid/triphenyl-phosphine is described at room temperature. Availability of the reagents and easy workup of the reaction make this method attractive for organic chemists.
- Entezari, Najmeh,Akhlaghinia, Batool,Rouhi-Saadabad, Hamed
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p. 201 - 206
(2015/02/05)
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- A facile one-pot synthesis and heterocyclisation of (R)-2-amino-3- ((aroylcarbamothioyl)thio)propanoic acids
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A series of (R)-2-amino-3-((aroylcarbamothioyl)thio)propanoic acid derivatives have been synthesised by a one-pot, threecomponent reaction of L-cysteine with ammonium thiocyanate in the presence of various acid chlorides under solvent-free conditions in excellent yields. These compounds were converted to (R)-2-thioxothiazolidine-4-carboxylic acid in water under reflux conditions.
- Mohebat, Razieh,Kafrizi, Elahe
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p. 172 - 174
(2014/04/17)
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- New aminobenzenesulfonamide-thiourea conjugates: Synthesis and carbonic anhydrase inhibition and docking studies
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A variety of 1-substituted-3-(3-aminosulfonylphenyl)thioureas (3a-k) and two new 1-aroyl-3-(4-aminosulfonylphenyl)thiourea derivatives (5a and 5b) were synthesized by reaction of 3-aminobenzenesulfonamide and 4- aminobenzenesulfonamide respectively with f
- Zaib, Sumera,Saeed, Aamer,Stolte, Karin,Fl?rke, Ulrich,Shahid, Mohammad,Iqbal, Jamshed
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p. 140 - 150
(2014/04/17)
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- SAR analysis of a series of acylthiourea derivatives possessing broad-spectrum antiviral activity
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A series of acylthiourea derivatives were designed, synthesized, and evaluated for broad-spectrum antiviral activity with selected viruses from Poxviridae (vaccinia virus) and two different genera of the family Bunyaviridae (Rift Valley fever and La Cross
- Burgeson, James R.,Moore, Amy L.,Boutilier, Jordan K.,Cerruti, Natasha R.,Gharaibeh, Dima N.,Lovejoy, Candace E.,Amberg, Sean M.,Hruby, Dennis E.,Tyavanagimatt, Shanthakumar R.,Allen III, Robert D.,Dai, Dongcheng
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scheme or table
p. 4263 - 4272
(2012/07/17)
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- IN VTRO ANTIBACTERIAL AND ANTIVIRAL ACTIVITIES OF SOME NOVEL 1,3,4-THIADIAZOLE DERIVATIVES
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A series of new 2-(substituted benzoylthiocarbamido)-5-(phenyl/sulphonamido)-1,3,4-thiadiazoles 4(a-g) and 5(a-g) were synthesized as potential antibacterial and antiviral compounds. 1,3,4-Thiadiazole compounds were prepared by the reaction of 2-amino-1,3,4-thiadiazoles with a solution containing ammonium thiocyanae and substituted benzoyl chloride in acetone/tetrahydrofuran. The structures of the synthesized compounds were confirmed using the elemental analysis and spectroscopic techniques such as IR, 1H NMR and Mass. The newly synthesized compounds were evaluated for in vitro antimicrobial activities by broth micro dilution method. Evaluation of the antiviral activity of the compounds against HIV-1 strain IIIB and HIV-2 strain (ROD) in MT-4 cells was performed using the MTT assay method.
- Dixit, Sheshagiri,Gadaginamath, G. S.,Joshi, S. D.,Kulkarni, V. H.,More, Uttam A.
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p. 109 - 114
(2020/12/09)
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- Three-component reaction between 4-hydroxycoumarin, ammonium thiocyanate and acid chlorides in the presence of N-methylimidazole under solvent-free conditions
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A novel method for oxazine ring formation is established using the reaction of ammonium thiocyanate and acid chlorides with 4-hydroxy coumarin in the presence of N-methylimidazole to afford oxazine derivatives in excellent yields.
- Hassanabadi, Alireza,Mosslemin, Mohammad H.,Tadayonfar, Seyd Ehsan
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experimental part
p. 29 - 31
(2011/04/26)
-
- Three-component reaction between 6-amino-N,N′ - Dimethyluracil and ammonium thiocyanate in the presence of aroyl chlorides under solvent-free conditions
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A novel method for the pyrimidine ring formation is established using the reaction of ammonium thiocyanate and aroyl chlorides with 6-amino-N,N′ -dimethyluracil under solvent-free conditions to afford the functionalized pyrimido[4,5-d]pyrimidines in excel
- Mohebat, Razieh,Mosslemin, Mohammad H.,Dehghan-Darehshiri, Ali,Hassanabadi, Alireza
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experimental part
p. 557 - 561
(2012/04/23)
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- Synthesis, characterization of some new 1-aroyl-3-(4-aminosulfonylphenyl) thioureas and crystal structure of 1-(3,4,5-trimethoxybenzoyl)- 3-(4-aminosulfonylphenyl)thiourea
-
A small library of novel 1-aroyl-3-(4-aminosulfonylphenyl)thiourea derivatives was synthesized by the reaction of sulfanilamide with substituted aroyl isothiocyanates in dry acetonitrile. The scope of the reaction was indicated by the synthesis of 1-undecanoyl-3-(4-aminosulfonylphenyl)thiourea, an acyl derivative involving alkanoyl isothiocyanate. All the compounds have been characterized by analytical and spectroscopic methods and in one case by single-crystal X-ray diffraction data.
- Saeed, Aamer,Mumtaz, Amara,Ishida
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experimental part
p. 45 - 54
(2012/01/06)
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- Design and synthesis of indole, 2,3-dihydro-indole, and 3,4-dihydro-2H-quinoline-1-carbothioic acid amide derivatives as novel HCV inhibitors
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An efficient synthetic methodology to provide indole, 2,3-dihydro-indole, and 3,4-dihydro-2H-quinoline-1-carbothioic acid amide derivatives is described. These conformationally restricted heterobicyclic scaffolds were evaluated as a novel class of HCV inhibitors. Introduction of an acyl group at the NH2 of the thiourea moiety has been found to enhance inhibitory activity. The chain length and the position of the alkyl group on the indoline aromatic ring markedly influenced anti-HCV activity. The indoline scaffold was more potent than the corresponding indole and tetrahydroquinoline scaffolds and analogue 31 displayed excellent activity (EC50 = 510 nM) against HCV without significant cytotoxicity (CC50 >50 μM).
- Kang, Iou-Jiun,Wang, Li-Wen,Hsu, Sheng-Ju,Lee, Chung-Chi,Lee, Yen-Chun,Wu, Yen-Shian,Hsu, Tsu-An,Yueh, Andrew,Chao, Yu-Sheng,Chern, Jyh-Haur
-
scheme or table
p. 4134 - 4138
(2010/04/26)
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- Efficient synthesis of 1-(5′-acylamino-1′,3′,4′- thiadiazol-2′-yl)-4-acyl-thiosemicarbazides
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Acyl chlorides reacted with ammonium thiocyanate and carbonic dihydrazide under phase-transfer catalysis to first afford 2,2′- bis(acylaminothiocarbonyl)-carbonic dihydrazides, which further cyclized in the presence of glacial acetic acid to efficiently give 1-(5′-acylamino- 1′,3′,4′-thiadiazol-2′-yl)-4-acyl-thiosemicarbazides in high yield. Copyright Taylor & Francis Group, LLC.
- Li, Zheng,Yang, Jing-Ya,Wang, Xi-Cun
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p. 2355 - 2362
(2007/10/03)
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- An efficient synthesis of polymethylene-bis-aroyl thiourea derivatives under the condition of phase-transfer catalysis
-
Reaction of polymethylene diamine with aroyl chloride and ammonium thiocyanate under the condition of solid-liquid phase-transfer catalysis using polyethylene glycol-400 (PEG-400) as the catalyst yielded polymethylene-bis- aroyl thiourea derivatives 3a-q
- Zhang, You-Ming,Wei, Tai-Bao,Xian, Liang,Gao, Li-Ming
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p. 2007 - 2013
(2007/10/03)
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- An efficient synthesis of polymethylene-bis-aroyl thiourea derivatives under the condition of phase transfer catalysis
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Reaction of polymethylene diamine with aroyl chloride and ammonium thiocyanate under the condition of solid-liquid phase transfer catalysis using polyethylene glycol-400(PEG-400) as the catalyst yielded polymethylene- bis-aroyl thiourea derivatives 3a - 3
- Wei, Tai-Bao,Zhang, You-Ming,Gao, Li-Ming
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p. 493 - 500
(2007/10/03)
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- Phase transfer catalyzed synthesis of arene-bis-aroyl thiourea derivatives
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Reaction of arene diamines with aroyl chloride and ammonium thiocyanate under the condition of solid-liquid phase transfer catalysis using polyethylene-glycol-600 (PEG-600) as the catalyst furnishes arene-bis-aroyl thioureas 3a-I in good to excellent yiel
- Zhang,Wei,Gao
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p. 700 - 702
(2007/10/03)
-
- Phase transfer catalyzed synthesis of 1,6- diaroyldithiohydrazodicarbonamide derivatives
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Reaction of hydrazine hydrate with aroyl chloride and ammonium thiocyanate under the condition of solid-liquid phase transfer catalysis using polyethylene glycol-600 (PEG-600) as the catalyst yielded 1,5- diaroyldithiohydrazodicarbonamides 3a - 3h in good to excellent yield.
- Zhang, Youming,Wei, Taibao,Lu, Jinren
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p. 3243 - 3248
(2007/10/03)
-
- Synthesis of n-aroyl-n'-hydroxyethyl (hydroxyphenyl)thiourea derivatives under the condition of phase transfer catalysis
-
Reaction of aminoethanol or aminophenol with aroyl chloride and ammonium thiocyanate under the condition of solid-liquid phase transfer catalysis using polyethylene glycol-600 (PEG-600) as the catalyst yielded N-aroyl-N'- hydroxyethyl(hydroxy phenyl)thiou
- Wei, Taibao,Zhang, Youming
-
p. 2851 - 2859
(2007/10/03)
-
- Flexible 1-[(2-aminoethoxy)alkyl]-3-ar(o)yl(thio)ureas as novel acetylcholinesterase inhibitors. Synthesis and biochemical evaluation
-
A series of flexible 1-(2-aminoethoxy)-3-ar(o)yl(thio)ureas was synthesized and assessed for antiacetylcholinesterase activity. This series was designed in order to optimize the spacer length linking the two pharmacophoric moieties, i.e., the basic nitrog
- Vidaluc,Calmel,Bigg,Carilla,Briley
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p. 2969 - 2973
(2007/10/02)
-