Synthesis and SAR of Some New 4 Substituted 3H-1,2,3,5-oxathiadiazole 2-Oxides as Antifungal Agents

被引：8

作者：

Sangshetti, Jaiprakash N. ^{[1
]}

Shinde, Devanand B. ^{[1
]}

机构：

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

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2010年 / 7卷 / 03期

关键词：

1,2,3,5-Oxathiadiazole 2-oxides; Amidoxime; 1,2,3 triazole; Piperidine; Antifungal activity; MIC values; SAR; ANTIBACTERIAL ACTIVITY; DERIVATIVES; ACID;

D O I：

10.2174/157018010790596696

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new series of 4-substituted 3H-1,2,3,5-oxathiadiazole 2-oxides bearing 1,2,3 triazole and piperidine ring has been synthesized in one step from amidoxime using thionyl chloride (SOCl2) and Triethylamine (TEA). All the synthesized compounds (10a-101) are new and evaluated for their in vitro antifungal activities using standard agar plate method. SAR for the series has been developed by comparing their MIC values with miconazole and fluconazole. Compound 10j from the series was equipotent with miconazole against C. albicans and F. oxysporum whereas activity of compound 10i was comparable to miconazole against F. oxysporum and C. neoformans (MIC-30 mu g/mL).

引用

页码：171 / 175

页数：5

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