Synthesis and anti-Candidal activity of N-(4-aryl/cyclohexyl)-2-(pyridine-4-yl carbonyl) hydrazinecarbothioamide
作者： Mashooq Ahmad Bhat , Abdul Arif Khan , Shahanavaj Khan , Mohamed A. Al-Omar , Mohammad Khalid Parvez
DOI: 10.1016/J.BMCL.2014.01.060
关键词:
摘要: Abstract 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 p-chloro (2c), p-iodo (2q), m-chloro (2l) o-nitro (2r) substitution at phenyl ring thiosemicarbazide enhanced the anti-Candida activity. Compound (2c) bearing p-cholorophenyl was found to be most effective albicans ATCC 66027, 12810 (blood) 178 (HVS) MIC value 0.09–0.78 μg/mL, whereas itraconazole exhibits inhibitory activity 0.04–1.56 μg/mL all tested strains. There is a correlation between anti-Candidal thiosemicarbazide. All synthesized compounds investigated for their potential cytotoxicity non cancer cell line MCF-10A. The active 2c, 2r 2a further cytotoxic effects on three lines; HT1080 (skin), HepG2 (liver) A549 (lung). showed minimal lines. Moreover, compound 2c displaying better C. ATCC66027 [blood] reference drug (itraconazole), represents good lead development newer, potent broad spectrum agents.
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