Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 2, Pages 742-745Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.11.048
Keywords
One pot synthesis; 1,2,4-Triazines; Hydrazides; 1,2,3-Triazole; Piperidine; MIC values; SAR
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Funding
- Council for Scientific and Industrial Research (CSIR), New Delhi
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An improved protocol for the synthesis of a novel series of 1,2,4-triazines possessing 1,2,3-triazole and piperidine ring using 1-(1-substituted piperidin-4-yl)-1H-1,2,3-triazole-4-carbohydrazide, benzil, ammonium acetate and ZrOCl2 center dot 8H(2)O as a catalyst in ethanol-water has been presented. The yields obtained are in the range of 87-94%. All the synthesized compounds (4a-4l) are novel and were evaluated for their in vitro antifungal activity. SAR for the series has been developed by comparing their MIC values with miconazole and fluconazole. Based on activity data SAR for the series has been developed. Compound 4c from the series was equipotent to miconazole against Candida albicans (MIC-25), Aspergillus niger (MIC-12.5) and Cryptococcus neoformans (MIC-25). Compound 4d was equipotent with miconazole against all tested organisms except Cryptococcus neoformans. Also compound 4i was equipotent with miconazole against C. albicans, A. niger and Fusarium oxysporum. (C) 2009 Elsevier Ltd. All rights reserved.
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