26416-42-2Relevant academic research and scientific papers
Synthetic nicotinic/isonicotinic thiosemicarbazides: In vitro urease inhibitory activities and molecular docking studies
Ali, Basharat,Mohammed Khan, Khalid,Arshia,Kanwal,Hussain, Shafqat,Hussain, Safdar,Ashraf, Muhammad,Riaz, Muhammad,Wadood, Abdul,Perveen, Shahnaz
, p. 34 - 45 (2018/05/09)
Nicotinic and isonicotinic thiosemicarbazide or hydrazine carbothioamides 3–27 were synthesized and the structures of synthetic compounds were elucidated by various spectroscopic techniques such as EI-MS, 1H-, and 13C NMR. Synthetic derivatives were evaluated for their urease inhibitory activity which revealed that except few all derivatives demonstrated excellent inhibition in the range of IC50 values of 1.21–51.42 μM as compared to the standard thiourea (IC50 = 21.25 ± 0.13 μM). Among the twenty-five synthetic derivatives nineteen 1–5, 7, 8, 10, 12, 14–18, 20–22, 24–27 were found to be more active showing IC50 values between 1.13 and 19.74 μM showing superior activity than the standard. Limited structure-activity relationship demonstrated that the positions of substituent as well as position of nitrogen in pyridine ring are very important for inhibitory activity of this class of compound. To verify these interpretations, in silico study was also performed. A good correlation was obtained between the biological evaluation of active compounds and docking study.
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
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.
