Synthesis of novel 3-(1-(1-substituted piperidin-4-yl)-1H-1,2,3-triazol-4-yl)-1,2,4-oxadiazol-5(4H)-one as antifungal agents

被引：89

作者：

Sangshetti, Jaiprakash N. ^{[1
]}

Nagawade, Rahul R. ^{[1
]}

Shinde, Devanand B. ^{[1
]}

机构：

[1] Dr Babasaheb Ambedkar Marathwada Univ, Dept Chem Technol, Aurangabad 431004, Maharashtra, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 13期

关键词：

1,2,3-Triazole; Piperidine; 1,2,4-Oxadiazole; MIC values; SAR; ANTIBACTERIAL ACTIVITY; DERIVATIVES;

D O I：

10.1016/j.bmcl.2009.04.134

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of 1,2,3 triazole compounds possessing 1,2,4 oxadiazole ring were efficiently synthesized. Synthesized compounds were evaluated for their in vitro antifungal activities using standard cup plate method. SAR for the series has been developed by comparing their MIC values with miconazole and fluconazole. Compound 11a from the series was more potent than miconazole against Candida albicans (MIC-20) and Aspergillus flavus (MIC-10) whereas equipotent with miconazole against Fusarium oxysporum (MIC-25) and Aspergillus niger (MIC-12.5). Also compound 11h was more potent than miconazole against Candida albicans (MIC-20) and Aspergillus niger (MIC-10) and equipotent with miconazole against Fusarium oxysporum. Compound 11h was equipotent with fluconazole against Aspergillus niger (MIC-10). (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：3564 / 3567

页数：4

共 27 条

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