Fluconazole analogues containing 2H-1,4-benzothiazin-3(4H)-one or 2H-1,4-benzoxazin-3(4H)-one moieties, a novel class of anti-Candida agents

被引：51

作者：

Borate, Hanumant B. ^{[1
]}

Maujan, Suleman R. ^{[1
]}

Sawargave, Sangmeshwer P. ^{[1
]}

Chandavarkar, Mohan A. ^{[2
]}

Vaiude, Sharangi R. ^{[2
]}

Joshi, Vinay A. ^{[2
]}

Wakharkar, Radhika D. ^{[1
]}

Iyer, Ramki ^{[2
]}

Kelkar, Ramesh G. ^{[1
]}

Chavan, Subhash P. ^{[1
]}

Kunte, Sunita S. ^{[1
]}

机构：

[1] Natl Chem Lab, Div Organ Chem, Pune 411008, Maharashtra, India

[2] FDC Ltd, Bombay 400102, Maharashtra, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 02期

关键词：

Antifungal; Fluconazole; Benzothiazinone; Benzoxazinone; TRIAZOLE DERIVATIVES SYNTHESIS; ANTIFUNGAL ACTIVITY; CANDIDA-ALBICANS; AZOLE DERIVATIVES; 1,4-BENZOTHIAZINE;

D O I：

10.1016/j.bmcl.2009.11.071

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

As a part of our program to develop new antifungal agents, a series of fluconazole analogues was designed and synthesized wherein one of the triazole moieties in fluconazole was replaced with 2H-1,4-benzothiazin-3(4H)-one or 2H-1,4-benzoxazin-3(4H)-one moiety. The new chemical entities thus synthesized were screened against various fungi and it was observed that the compounds 4a and 4i are potent inhibitors of Candida strains. The structure-activity relationship for these compounds is discussed. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：722 / 725

页数：4

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