期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 2, 页码 722-725出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.11.071
关键词
Antifungal; Fluconazole; Benzothiazinone; Benzoxazinone
资金
- CSIR, New Delhi
- Department of Science and Technology, New Delhi
- FDC Ltd, Mumbai
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.
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