TY - JOUR T1 - 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 JF - Bioorganic & Medicinal Chemistry Letters Y1 - 2010 A1 - Borate, Hanumant B. A1 - Maujan, Suleman R. A1 - Sawargave, Sangmeshwer P. A1 - Chandavarkar, Mohan A. A1 - Vaiude, Sharangi R. A1 - Joshi, Vinay A. A1 - Wakharkar, Radhika D. A1 - Iyer, Ramki A1 - Kelkar, Ramesh G. A1 - Chavan, Subhash P. A1 - Kunte, Sunita S. KW - antifungal KW - Benzothiazinone KW - Benzoxazinone KW - Fluconazole AB -

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.

PB - PERGAMON-ELSEVIER SCIENCE LTD CY - THE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLAND VL - 20 IS - 2 U3 - Foreign U4 - 2.661 ER -