97195-92-1Relevant academic research and scientific papers
Synthesis, molecular docking, and evaluation of antibacterial activity of 1,2,4-triazole-norfloxacin hybrids
Yang, Ping,Luo, Jia-Bao,Wang, Zi-Zhou,Zhang, Li-Lei,Feng, Jin,Xie, Xiao-Bao,Shi, Qing-Shan,Zhang, Xin-Guo
, (2021/09/04)
A series of 1,2,4-triazole-norfloxacin hybrids was designed, synthesized, and evaluated for in vitro antibacterial activity against common pathogens. All the newly synthesized compounds were characterized by Fourier-transform infrared spectrophotometry, p
Synthesis and molecular docking studies of glucose-linked isonicotinoyl- 1, 3, 4-thiadiazolidines as antitubercular agents
Chavan, Snehal A.,Ulhe, Avinash G.,Berad, Baliram N.,Chikhale, Rupesh V.
, p. 15 - 22 (2018/03/05)
Background: The recent emergence of multidrug-resistant strains of M. tuberculosis that are resistant to two major effective drugs, viz. isoniazid and rifampicin, stimulated us to make an attempt for the development of a new class of potent antitubercular
Synthesis and antimicrobial activity of some new 1,2,4-trizoles
Jain, Rakesh Kumar,Mishra, Vikash Kumar,Kashaw, Varsha
, p. 1317 - 1322 (2017/05/02)
A series of 1,2,4-triazole derivatives were synthesized using appropriate synthetic route and structures were confirmed by IR,1H NMR and elemental analysis. All the synthesized compounds (6a-6h and 7a-7h) were evaluated for antimicrobial activity by determining their minimum inhibitory concentrations (MICs) against a panel of Gram-positive, Gram-negative bacteria and fungi. Most of the compounds showed significant antimicrobial activity against Gram-positive bacteria viz. S. aureus, B. subtilis, Gram-negative bacteria viz. E. coli, P. aerugenosa and fungi viz. C. albicans, A. niger. Some of the compounds showed better antibacterial activities against Gram-positive bacteria compared to Gram-negative bacteria. Compounds 7g, 6g, 6a exhibited good MICs against Gram-positive bacteria and 7f showed better MICs against Gram-negative bacteria compared to reference norfloxacin. Compounds 7f and 7d exhibited MICs which is equipotent to the reference drug ketoconazole.
Synthesis and anticancer evaluation of 1,3,4-oxadiazoles, 1,3,4-thiadiazoles, 1,2,4-triazoles and mannich bases
Megally Abdo, Nadia Youssef,Kamel, Mona Monir
, p. 369 - 376 (2015/06/17)
A series of 5-(pyridin-4-yl)-N-substituted-1,3,4-oxadiazol-2-amines (3a-d), 5-(pyridin-4-yl)-N-substituted- 1,3,4-thiadiazol-2-amines (4a-d) and 5-(pyridin-4-yl)-4-substituted-1,2,4-triazole-3-thiones (5a-d) were obtained by the cyclization of hydrazinecarbothioamide derivatives 2a-d derived from isonicotinic acid hydrazide. Aminoalkylation of compounds 5a-d with formaldehyde and various secondary amines furnished the Mannich bases 6a-p. The structures of the newly synthesized compounds were confirmed on the basis of their spectral data and elemental analyses. All the compounds were screened for their in vitro anticancer activity against six human cancer cell lines and normal fibroblast cells. Sixteen of the tested compounds exhibited significant cytotoxicity against most cell lines. Among these derivatives, the Mannich bases 6j, 6m and 6p were found to exhibit the most potent activity. The Mannich base 6m showed more potent cytotoxic activity against gastric cancer NUGC (IC50=0.021 μM) than the standard CHS 828 (IC50=0.025 μM). Normal fibroblast cells WI38 were affected to a much lesser extent (IC50>10 μM).
Synthesis and antitumor activity of 4-cyclohexyl/aryl-5-(pyridin-4-yl)-2,4-dihydro-3H-1,2,4-triazole-3-thiones
Bhat, Mashooq Ahmad,Al-Omar, Mohamed A.,Naglah, Ahmed M.,Abdulla, Mohamed M.,Fun, Hoong-Kun
, p. 1558 - 1567 (2015/04/21)
The reaction of 2-isonicotinoyl-N-cyclohexyl/arylhydrazinecarbothioamide (2a-r) with sodium hydroxide, in each case, a single product was obtained. The structures of the compounds were confirmed on the basis of their elemental analysis and spectral data.
Synthesis and anti-Candidal activity of N-(4-aryl/cyclohexyl)-2-(pyridine- 4-yl carbonyl) hydrazinecarbothioamide
Bhat, Mashooq Ahmad,Khan, Abdul Arif,Khan, Shahanavaj,Al-Omar, Mohamed A.,Parvez, Mohammad Khalid,Al-Dosari, Mohammed Salem,Al-Dhfyan, Abdullah
, p. 1299 - 1302 (2014/03/21)
Eighteen N-(4-aryl/cyclohexyl)-2-(pyridine-4-yl carbonyl) hydrazinecarbothioamide derivatives were synthesized, evaluated against ten clinical isolates of Candida spp. and compared with itraconazole. Introduction of p-chloro (2c), p-iodo (2q), m-chloro (2
AZOLE DERIVATIVES AS WTN PATHWAY INHIBITORS
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Page/Page column 61-62, (2010/12/29)
The present invention relates to new compounds of formula I, to processes for their preparation, to pharmaceutical formulations containing such compounds and to their use in therapy. Such compounds find particular use in the treatment and/or prevention of conditions or diseases which are affected by over-activation of signaling in the Wnt pathway. For example, these may be used in preventing and/or retarding proliferation of tumor cells, for example carcinomas such as colon carcinomas.
Synthesis and anticonvulsant activity of substituted oxadiazole and thiadiazole derivatives
Yar, Mohammad Shahar,Akhter, Mohammad Wasim
experimental part, p. 393 - 397 (2010/01/13)
A series of five membered heterocyclics was synthesized by the reaction between isoniazid and various substituted isothiocyanates and was tested for their anticonvulsant activity by determining their ability to provide protection against convulsions induc
Synthesis and molecular structure of new S-nucleosides of 5-(4-pyridyl)-4-aryl-4H-1,2,4-triazole-3-thiols
Zhang, Huan-Huan,Hu, Xiu-Qin,Fan, Gui-Fang,Xu, Peng-Fei
body text, p. 834 - 841 (2009/12/01)
The synthesis of some new S-nucleosides of 5-(4-pyridyl)-4-aryl-4H-l,2,4- triazole-3-thiols (4a-n) is described. Direct glycosylation of (4a-n) with tetra-O-acetyl-α-D-glucopyranosyl bromide in the presence of potassium hydroxide followed by deacetylation using dry ammonia in methanol gave the corresponding 3-S-(β-D-glucopyranosyl)-5-(4-pyridyl)-4-aryl-4H-l,2,4- triazoles (6a-n) in good yields. All the compounds were fully characterized by means of 1H NMR, 13C NMR spectra and elemental analyses. To assist in the interpretation of the spectroscopic data, the crystal structure of 3-S-(2′,3′,4′,6′-tetra-O-acetyl-β-D- glucopyranosyl)-5-(4-pyridyl)-4-phenyl-4H-l,2,4-triazole (5a) was determined by X-ray diffraction.
Novel anthelmintic and insecticidal compositions
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Page/Page column 9, (2008/06/13)
The present invention relates to novel anthelmintic and insecticidal compositions in general, and, more specifically, compositions containing triazole derivatives as active ingredients.
