- Microwave irradiation synthesis of novel indole triazole Schiff base fluorescent probe for Al3+ ion
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An efficient triazole Schiff base fluorescent Al3+-probe 4-((2-hydroxybenzylidene) amino)-5-(1H-indol-3-yl)-4H-1,2,4-triazole-3-thiol (H2L) was designed and synthesized under microwave irradiation. The structure of fluorescent probe H2L was characterized by spectral data and elemental analysis. The probe H2L displays excellent chemo-selectivity towards Al3+ over other metal ions, which can directly inspect with the naked eye under UV lamp. The limit of detection of the probe H2L for Al3+ could reach 29.9 nM. The binding stoichiometry between H2L and Al3+ was determined from the Job's plot to be 1:1, the association constant (Ka) of 9.31 × 104 M?1, and further verified with fluorescence titration, ESI-MS and 1H NMR study.
- Shi, Zhichuan,Zhao, Zhigang
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- Synthesis and functionalization of the 3-(1, 3, 4-oxadiazol-2-yl)-1H- indoles
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A modified method is proposed for the preparative synthesis of 3-(1, 3, 4-oxadiazol-2-yl)-1H-indoles in high yield. We are the first to demonstrate the functionalization of this heterocyclic system by alkylation. In particular, syntheses are reported for [3-(1, 3, 4-oxadiazol-2-yl)-1H-indol-1-yl]acetic acids and their amide derivatives.
- Alyab'ev,Kravchenko,Ivashchenko
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- Development of 2-oindolin-3-ylidene-indole-3-carbohydrazide derivatives as novel apoptotic and anti-proliferative agents towards colorectal cancer cells
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Mitochondrial anti-apoptotic Bcl2 and BclxL proteins, are overexpressed in multiple tumour types, and has been involved in the progression and survival of malignant cells. Therefore, inhibition of such proteins has become a validated and attractive target for anticancer drug discovery. In this manner, the present studies developed a series of novel isatin–indole conjugates (7a-j and 9a-e) as potential anticancer Bcl2 and BclxL inhibitors. The progression of the two examined colorectal cancer cell lines was significantly inhibited by all of the prepared compounds with IC50 ranges132–611 nM compared to IC50 = 4.6 μM for 5FU, against HT-29 and IC50 ranges 37–468 nM compared to IC50 = 1.5 μM for 5FU, against SW-620. Thereafter, compounds 7c and 7g were selected for further investigations. Interestingly, both compounds exhibited selective cytotoxicity against both cell lines with high safety to normal fibroblast (HFF-1). In addition, both compounds 7c and 7g induced apoptosis and inhibited Bcl2 and BclxL expression in a dose-dependent manner. Collectively, the high potency and selective cytotoxicity suggested that conjugates 7c and 7g could be a starting point for further optimisation to develop novel pro-apoptotic and antitumor agents towards colon cancer.
- Abdel-Aziz, Hatem A.,Abdulla, maha,Abo-Ashour, mahmoud f.,Ahmad, Rehan,Al-Khayal, Khayal,Al-Rashood, Sara T.,Al-Warhi, Tarfah,Alharbi, Amal,Ayyad, Rezk R.,El-Haggar, Radwan,Eldehna, Wagdy m.
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- Synthesis and biological evaluation of novel 4,5-bisindolyl-1,2,4-Triazol-3- ones as glycogen synthase kinase-3β inhibitors and neuroprotective agents
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A series of novel 4,5-bisindolyl-1,2,4-Triazol-3-ones were designed, prepared and evaluated for their glycogen synthase kinase (GSK)-3β inhibitory activities. Compounds exhibited favorable inhibitory potency towards GSK-3β kinase at the molecular level and in cells indicated by significantly reducing GSK-3β substrate Tau phosphorylation at Ser396 in primary neurons showing the inhibition of cellular GSK-3β. In an in vitro model of neuronal injury, compounds 6b, 6d and 6f prevented glutamate-induced neuronal death which was closely associated with cerebral ischemic stroke. Preliminary structure-Activity relationship was examined and showed that different substituents on the indole ring had significant influences on the GSK-3β inhibitory potency. These findings may provide new insights into the development of novel GSK-3β inhibitors as neuroprotective agents.
- Hu, Yuanyuan,Ruan, Wenchen,Gao, Anhui,Zhou, Yubo,Gao, Lixin,Xu, Meng,Gao, Jianrong,Ye, Qing,Li, Jia,Pang, Tao
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- Design of balanced COX inhibitors based on anti-inflammatory and/or COX-2 inhibitory ascidian metabolites
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The aim of this study was to design and synthesize COX-1/COX-2 balanced inhibitors incorporating the structural motifs of anti-inflammatory ascidian metabolites. We designed a series of substituted indole analogs that incorporate the key structures of the ascidian metabolites, herdmanines C and D. The synthesized analogs were tested for their inhibitory activity against COX-1 and COX-2, and compound 5m, which displayed balanced inhibition, was further evaluated for in vitro anti-inflammatory activity. Compound 5m suppressed the expression of pro-inflammatory factors, including iNOS, COX-2, TNF-α, and IL-6 in LPS-stimulated murine RAW264.7 macrophages. The reduction of PGE2, NO, and ROS was also observed, together with the suppression of NF-κB, IKK, and IκBα phosphorylation. Our results characterized 5m as a COX-1/COX-2 balanced inhibitor that subsequently caused ROS inhibition and NF-κB suppression, and culminated in the suppression of iNOS, COX-2, TNF-α, and IL-6 expression.
- Ju, Zhiran,Su, Mingzhi,Hong, Jongki,La Kim, Eun,Moon, Hyung Ryong,Chung, Hae Young,Kim, Suhkmann,Jung, Jee H.
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- Diversity-oriented synthesis and antifungal activities of novel pimprinine derivative bearing a 1,3,4-oxadiazole-5-thioether moiety
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Abstract: Based on the strategy of diversity-oriented synthesis and the structures of natural product pimprinine and streptochlorin, two series of novel pimprinine derivatives containing 1,3,4-oxadiazole-5-thioether moieties were efficiently synthesized under the optimized reaction conditions. Biological assays conducted at Syngenta showed the designed derivatives displayed an altered pattern of biological activity, of which 5h was identified as the most promising compound with strong activity against Pythium dissimile and also a broad antifungal spectrum in primary screening. Further structural optimization of pimprinine and streptochlorin derivatives is well under way, aiming to discover synthetic analogues with improved antifungal activity. Graphic abstract: Two series of novel pimprinine derivatives containing 1,3,4-oxadiazole-5-thioether moieties wereefficiently synthesized through diversity-oriented synthesis strategy under the optimizedconditions. Biological assays showed the designed derivatives exhibited potential activity.[Figure not available: see fulltext.].
- Song, Zi-Long,Zhu, Yun,Liu, Jing-Rui,Guo, Shu-Ke,Gu, Yu-Cheng,Han, Xinya,Dong, Hong-Qiang,Sun, Qi,Zhang, Wei-Hua,Zhang, Ming-Zhi
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- NOVEL INDOLE DERIVATIVES AND COMPOSITION FOR PREVENTING OR TREATING INFLAMMATORY DISEASES COMPRISING THE SAME
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The present invention relates to a novel indole derivative and a composition for preventing or treating inflammatory diseases comprising the same. More specifically, since a series of substituted indole derivative compounds combining a core structure of an anti-inflammatory seaweed metabolite are designed and synthesized, and inhibitory activity and anti-inflammatory activity on COX-1 and COX-2 in the compound are confirmed, the compound can be used as an effective pharmaceutical composition or health functional food composition for preventing, alleviating or treating inflammatory diseases.
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- Indole derivatives containing disulfide alkyl heterocyclic structure or stereoisomer, salt or solvate of the indole derivatives
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The invention relates to a preparation method and application of indole derivatives containing a disulfide alkyl heterocyclic structure. The compounds have a general structure as shown in a general formula (I) shown in the specification. Indole compounds
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Paragraph 0035; 0050-0052
(2020/07/06)
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- Design, Synthesis, and Pharmacological Evaluation of First-in-Class Multitarget N-Acylhydrazone Derivatives as Selective HDAC6/8 and PI3Kα Inhibitors
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Targeting histone deacetylases (HDACs) and phosphatidylinositol 3-kinases (PI3Ks) is a very promising approach for cancer treatment. This manuscript describes the design, synthesis, in vitro pharmacological profile, and molecular modeling of a novel class of N-acylhydrazone (NAH) derivatives that act as HDAC6/8 and PI3Kα dual inhibitors. The surprising selectivity for PI3Kα may be related to differences in the conformation in the active site. Cellular studies showed that these compounds act in HDAC6 inhibition and the PI3/K/AKT/mTOR pathway. The compounds that are selective for inhibition of HDAC6/8 and inhibit PI3Kα show potential for the treatment of cancer.
- Alves, Marina A.,Chaves, Lorrane S.,Fernandes, Patrícia D.,Fraga, Carlos A. M.,Guerra, Fabiana S.,Rodrigues, Daniel A.,Sagrillo, Fernanda S.,Sant'Anna, Carlos M. R.,Thota, Sreekanth,de Sena M. Pinheiro, Pedro
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supporting information
(2020/02/25)
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- Derivative containing 1, 2, 4-mercaptotriazole and preparation method and application of derivative
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The invention relates to the technical field of medicinal chemistry, in particular to a derivative containing 1, 2, 4-mercaptotriazole and a preparation method and application of the derivative. The derivative containing 1, 2, 4-mercaptotriazole has relatively good inhibitory activity on DCN1-UBC12 protein-protein interaction, so that the 1, 2, 4-mercaptotriazole derivative has relatively good inhibitory activity on DCN1-UBC12 protein-protein interaction. According to the record of the embodiment, compared with NAcM-COV, the derivative containing 1, 2, 4-mercaptotriazole provided by the invention has better inhibitory activity on DCN1-UBC12 protein-protein interaction, and the structural formula of the derivative containing 1, 2, 4-mercaptotriazole is shown in the specification.
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Paragraph 0152-0153
(2020/11/26)
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- Synthesis of novel indole derivatives containing double 1,3,4-oxadiazole moiety as efficient bactericides against phytopathogenic bacterium Xanthomonas oryzae
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Abstract: A series of novel indole derivatives containing double 1,3,4-oxadiazole moiety was designed, synthesized and evaluated for their antibacterial activities in vitro. These compounds were fully characterized by 1H NMR, 13C NMR, and HRMS. Bioassay results indicated that most of title compounds exhibited excellent antibacterial activities against rice bacterial pathogen Xanthomonas oryzae (Xoo). For example, compounds 7d, 7h, 7i, 7j, 7k, 7l and 7m had the half-maximal effective concentration (EC50) values of 52.31, 54.12, 40.65, 38.80, 51.13, 52.75 and 50.66?μg/mL, respectively, which was better than that of commercial product bismerthiazol (BMT) (85.18?μg/mL). The experimental results proved that indole derivatives bearing double 1,3,4-oxadiazole unit are promising candidates for the development of new agricultural bactericides against pathogenic bacterium Xoo. Graphical abstract: [Figure not available: see fulltext.].
- Tian, Kun,Li, Xiao-Qin,Zhang, Li,Gan, Yi-Yuan,Meng, Jiao,Wu, Shou-Qun,Wan, Jin-Lin,Xu, Yang,Cai, Chao-Ting,Ouyang, Gui-Ping,Wang, Zhen-Chao
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- A double-indole hydrazone compound and use thereof
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The invention provides a bisindole acylhydrazone compound shown as the formula I or salt, hydrate or crystals, accepted in the pharmacy, of the bisindole acylhydrazone compound. According to the bisindole acylhydrazone compound, R does not exist or is selected from alkylene of C1-5. The bisindole acylhydrazone compound has a certain antibacterial activity, and can serve as potential antibiotics or a daily chemical product. What is beyond the expectation is that compounds 4e-4h and compounds 4a-4c are quite similar in structure, the antibacterial activity of the compounds 4e-4h and the antibacterial activity of the compounds 4a-4c are obviously better than that of other compounds, particularly, the activity of the compound 4h is best and is remarkably better than that of compounds 4e-4g. The formula I is shown in the specification.
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Paragraph 0036; 0041
(2017/10/06)
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- Indole hydrazone compounds
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The invention provides a compound of the formula I as shown in the description. In the formula, R is connected with the carbon atom at the 2nd or 3rd site of indolyl and is selected from none or C1-3 alkylene. Molecular tweezers of bisindole acylhydrazone have a good recognition cooperation function on inspected malic acid, tartaric acid, ascorbic acid and tryptophan, and have no recognition cooperation function on other inspected organic acids such as lactic acid, oxalic acid, tyrosine, histidine and serine. Therefore, due to the selective recognition property of a molecular tweezers receptor has the potential to be applied to fields such as analysis and separation of relevant organic acids in biological medicines, and transportation of organic acid medicines.
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Paragraph 0039; 0040; 0043; 0044; 0046
(2017/11/17)
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- Development of Novel Bis(indolyl)-hydrazide-Hydrazone Derivatives as Potent Microtubule-Targeting Cytotoxic Agents against A549 Lung Cancer Cells
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The biological significance of microtubules makes them a validated target of cancer therapy. In this study, we have utilized indole, an important pharmacological scaffold, to synthesize novel bis(indolyl)-hydrazide-hydrazone derivatives (NMK-BH compounds) and recognized NMK-BH3 as the most effective one in inhibiting A549 cell proliferation and assembly of tissue-purified tubulin. Cell viability experiments showed that NMK-BH3 inhibited proliferation of human lung adenocarcinoma (A549) cells, normal human lung fibroblasts (WI38) and peripheral blood mononuclear cells (PBMC) with IC50 values of -2, 48.5, and 62 μM, respectively. Thus, the relatively high cytotoxicity of NMK-BH3 toward lung carcinoma (A549) cells over normal lung fibroblasts (WI38) and PBMC confers a therapeutic advantage of reduced host toxicity. Flow cytometry, Western blot, and immunofluorescence studies in the A549 cell line revealed that NMK-BH3 induced G2/M arrest, mitochondrial depolarization, and apoptosis by depolymerizing the cellular interphase and spindle microtubules. Consistent with these observations, study in cell free system revealed that NMK-BH3 inhibited the microtubule assembly with an IC50 value of -7.5 μM. The tubulin-ligand interaction study using fluorescence spectroscopy indicated that NMK-BH3 exhibited strong and specific tubulin binding with a dissociation constant of -1.4 μM at a single site, very close to colchicine site, on β-tubulin. Collectively, these findings explore the cytotoxic potential of NMK-BH3 by targeting the microtubules and inspire its development as a potential candidate for lung cancer chemotherapy.
- Das Mukherjee, Dipanwita,Kumar, N. Maruthi,Tantak, Mukund P.,Das, Amlan,Ganguli, Arnab,Datta, Satabdi,Kumar, Dalip,Chakrabarti, Gopal
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p. 3020 - 3035
(2016/06/14)
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- Design, synthesis and QSAR study of arylidene indoles as anti-platelet aggregation inhibitors
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A series of novel substituted indole carbohydrazide was synthesized and evaluated for anti-platelet aggregation activity. The structures of the synthesized compounds were confirmed by spectral data and elemental analysis and were evaluated for their ability to inhibit platelet aggregation induced by adenosine diphosphate, arachidonic acid (AA) and collagen. Compounds 3e and 3b exhibited the highest activities against the platelet aggregation induced by collagen with IC50 values of 12.7 and 13.3 μM, respectively, and 2h with IC50 value of 51.88 μM and 2i with IC50 of 44.38 μM efficiently inhibited platelet aggregation induced by AA. The QSAR investigation indicated the importance of the topological, constitutional and geometrical parameters (PW3, PW4, LP1 and GATS6v) in describing the anti-platelet aggregation activity of the synthesized hydrazides. Evaluation of cytotoxic activity of the compounds against L929 cell line and three cancer cell lines revealed that none of the compounds have significant cytotoxicity. Graphical Abstract: [Figure not available: see fulltext.]
- Mirfazli, Seyedeh Sara,Khoshneviszadeh, Mehdi,Jeiroudi, Mohammad,Foroumadi, Alireza,Kobarfard, Farzad,Shafiee, Abbas
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- Microwave-assisted synthesis and molecular recognition properties of novel indole acylhydrazone receptors
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Indole acylhydrazones were synthesised in high yields under microwave irradiation By using indole carboxylic acid and 1,4-benzenedialdehyde as starting materials. Their structures were characterised by 1H NMR, IR, MS spectra and elemental analysis. Selective recognition properties of these receptors have been investigated by UV-Vis spectra titration indicating that these receptors can form 1:1 supramolecular complexes with malic acid, tartaric acid, ascorbic acid and tryptophan.
- Ye, Ying,Suo, Yourui,Yang, Fang,Yang, Yongjing,Han, Lijuan
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p. 296 - 299
(2015/06/02)
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- Ultrasound-assisted, one-pot, three-component synthesis and antibacterial activities of novel indole derivatives containing 1,3,4-oxadiazole and 1,2,4-triazole moieties
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Thirteen novel indole derivatives were efficiently synthesized through ultrasound irradiation by using 4-amino-5-(1H-indol-3-yl)-4H-[1,2,4]triazole-3-thiol (8) and 2-mercapto-5-substituted-1,3,4-oxadiazoles (5a-m). Compared with conventional and microwave methods, yields increased to 82-93%, and reaction times decreased to 15-35 min. The structures of these novel compounds were characterized by spectral data and elemental analysis. Two out of the synthesized compounds (10f and 10l) exhibited excellent activity against Staphylococcus aureus and Escherichia coli, and thus warrant further research.
- Shi, Zhichuan,Zhao, Zhigang,Huang, Meiwei,Fu, Xiaolin
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p. 1320 - 1327
(2015/12/11)
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- Suprafenacine, an Indazole-hydrazide agent, target Cancer cells through microtubule destabilization
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Microtubules are a highly validated target in cancer therapy. However, the clinical development of tubulin binding agents (TBA) has been hampered by toxicity and chemoresistance issues and has necessitated the search for new TBAs. Here, we report the identification of a novel cell permeable, tubulin-destabilizing molecule - 4,5,6,7-tetrahydro-1H-indazole-3- carboxylic acid [1p-tolyl-meth-(E)-ylidene]-hydrazide (termed as Suprafenacine, SRF). SRF, identified by in silico screening of annotated chemical libraries, was shown to bind microtubules at the colchicine-binding site and inhibit polymerization. This led to G2/M cell cycle arrest and cell death via a mitochondria-mediated apoptotic pathway. Cell death was preceded by loss of mitochondrial membrane potential, JNK - mediated phosphorylation of Bcl-2 and Bad, and activation of caspase-3.Intriguingly, SRF was found to selectively inhibit cancer cell proliferation and was effective against drug-resistant cancer cells by virtue of its ability to bypass the multidrug resistance transporter P-glycoprotein. Taken together, our resultssuggest that SRF has potential as a chemotherapeutic agent for cancer treatment and provides an alternate scaffold for the development of improved anti-cancer agents.
- Choi, Bo-Hwa,Chattopadhaya, Souvik,Thanh, Le Nguyen,Feng, Lin,Nguyen, Quoc Toan,Lim, Chuan Bian,Harikishore, Amaravadhi,Reddy, Ravi Prakash,Bharatham, Nagakumar,Zhao, Yan,Liu, Xuewei,Yoon, Ho Sup
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supporting information
(2015/02/18)
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- Structure-activity relationship studies and biological characterization of human NAD+-dependent 15-hydroxyprostaglandin dehydrogenase inhibitors
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The structure-activity relationship (SAR) study of two chemotypes identified as inhibitors of the human NAD+-dependent 15-hydroxyprostaglandin dehydrogenase (HPGD, 15-PGDH) was conducted. Top compounds from both series displayed potent inhibition (IC50 2 production in A549 lung cancer and LNCaP prostate cancer cells.
- Duveau, Damien Y.,Yasgar, Adam,Wang, Yuhong,Hu, Xin,Kouznetsova, Jennifer,Brimacombe, Kyle R.,Jadhav, Ajit,Simeonov, Anton,Thomas, Craig J.,Maloney, David J.
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supporting information
p. 630 - 635
(2014/01/23)
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- TUBULIN INHIBITORS
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The present invention relates to a compound of Formula (I) for use as a medicament, wherein: m is 0, 1, 2, 3, 4, or 5; R1 and R2 together form a five-membered, six-membered, or seven-membered ring, wherein R1 and R2 together as a group is -(CH2)3-, -(CH2)4 -, or -(CH2)5-; R3 at each occurrence is independently selected from the group consisting of H, halogen, hydroxyl, alkoxy, and a substituted or unsubstituted C1-C5 alkyl; and R4 is H, halogen, or a substituted or unsubstituted C1-C5 alkyl
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Paragraph 00220; 00221; 00232
(2013/11/18)
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- Synthesis and antifungal activity of 3-(1,3,4-oxadiazol-5-yl)-indoles and 3-(1,3,4-oxadiazol-5-yl)methyl-indoles
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On the basis of the principle of combination of active structural moieties, a modified and efficient synthetic method for three series of novel indole-based 1,3,4-oxadiazoles is described. Bioassays conducted at Syngenta showed that several of the synthesized compounds exhibit higher antifungal activity than pimprinine, the natural product which inspired this synthesis. Two main structural alterations were found to broaden the spectrum of biological activity in most cases. Compounds 3g, 6c, 6e, 6h, 9d, 9e, 9h and 9m (Fig. 1) were identified as the most active on the biological assays, and will be studied further.
- Zhang, Ming-Zhi,Mulholland, Nick,Beattie, David,Irwin, Dianne,Gu, Yu-Cheng,Chen, Qiong,Yang, Guang-Fu,Clough, John
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- A series of 2-arylamino-5-(indolyl)-1,3,4-thiadiazoles as potent cytotoxic agents
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A series of 2-arylamino-5-(indolyl)-1,3,4-thiadiazoles 6a-v were prepared and studied for their anticancer activity against selected human cancer cell lines. The reaction of indolylhydrazides 3a-h with a variety of aryl isothiocyanates 4 afforded the key intermediate thiosemicarbazides 5a-v, which upon treatment with acetyl chloride produced the 2-arylamino-5-(indolyl)-1,3,4- thiadiazoles 6a-v in good yields. Most of the synthesized compounds showed selective cytotoxicity towards human breast cancer cell line (MDA-MB-231). Of the synthesized 2-arylamino-5-(indolyl)-1,3,4-thiadiazoles, compound 6f is the most potent towards tested cancer cell lines (IC50 = 0.15-1.18 μM).
- Kumar, Dalip,Kumar, N. Maruthi,Noel, Brett,Shah, Kavita
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p. 432 - 438
(2012/11/07)
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- Novel bis(indolyl)hydrazide-hydrazones as potent cytotoxic agents
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A series of bis(indolyl) hydrazide-hydrazones 5a-n were synthesized and evaluated for their cytotoxicity against selected human cancer cell lines. The reaction of indole-3-carboxaldehyde 2 with indole-3-carbohydrazide 4 in presence of catalytic amount of acetic acid afforded 5a-n in good yields. Among the synthesized bis(indolyl)hydrazide-hydrazones, the compound 5b with N-(p-chlorobenzyl) and bromo substituents was found to be the most potent against multiple cancer cell lines (IC50 = 1.0 μM, MDA-MB-231). The compound 5k exhibited selective cytotoxicity against breast cancer cell line MCF7 (IC50 = 3.1 μM).
- Kumar, Dalip,Maruthi Kumar,Ghosh, Soumitra,Shah, Kavita
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p. 212 - 215
(2012/03/10)
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- OXADIAZOLE DERIVATIVES AND THEIR USE AS NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS
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Oxadiazole derivatives of formula (I) where ring A is a bicyclic or tricyclic system. Claimed compounds are active on nicotinic acetylcholine receptors (nAChRs), and are useful to treat neurological, psychiatric, and gastrointestinal disorders, as well as sepsis and obesity.
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Page/Page column 46
(2009/07/17)
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- 4-SUBSTITUTED AZAADAMANTANE DERIVATIVES AND METHODS OF USE THEREOF
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The invention relates to compounds that are 4-substituted azaadamantane derivatives, compositions comprising such compounds, and methods of using such compounds and compositions.
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Page/Page column 35
(2008/12/04)
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- Fluorogenic and chromogenic β-lactamase substrates
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Chromogenic and fluorogenic substrates for β-lactamase, methods for synthesis thereof and methods for detecting β-lactamase in a sample are provided. The substrates are substantially colorless or substantially nonfluorescent β-lactam compounds which include an electronegative leaving group. The leaving group comprises a carbamate, carbonate, thiocarbamate or thiocarbonate linkage and a fluorescent moiety or a moiety capable of producing a visually detectable colored product. Upon cleavage of the lactam ring by β-lactamase, the leaving group is liberated and fluorescence or a colored product is produced.
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- SYNTHESIS OF FUNCTIONAL DERIVATIVES OF INDOLE-3-CARBOXYLIC ACIDS
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Methods are described for the synthesis of the esters, hydrazides, amidines, N-phenylamidines, N1-phenylamidrazones, N1-acylamidrazones, and amide oximes of indole-3-carboxylic and 1-methylindole-3-carboxylic acids.
- Kelarev, V. I.,Gasanov, S. Sh.,Karakhanov, R. A.,Polivin, Yu. N.,Kuatbekova, K. P.,Panina, M. E.
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p. 2069 - 2074
(2007/10/02)
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- Synthesis and properties of azoles and their derivatives. 33. Synthesis of 1,3,4-oxadiazoles that contain an indolyl group
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2,5-Disubstituted oxadiazoles with indole residues were synthesized by condensation of the hydrochlorides of the corresponding imido esters with hydrazines, as well as by cyclization of hydrazides by the action of POCl3. 2-Substituted oxadiazoles of the same series were obtained by condensation of the corresponding hydrazides with ethyl orthoformate.
- Kelarev,Shvekhgeimer
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p. 258 - 261
(2007/10/02)
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