title: 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.
abstract: 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.
authors: Division of Organic Chemistry, National Chemical Laboratory, Dr. Homi Bhabha Road, Pune 411 008, India. hb.borate@ncl.res.in
authors: Hanumant B
authors: HB
authors: Borate
authors: Suleman R
authors: SR
authors: Maujan
authors: Sangmeshwer P
authors: SP
authors: Sawargave
authors: Mohan A
authors: MA
authors: Chandavarkar
authors: Sharangi R
authors: SR
authors: Vaiude
authors: Vinay A
authors: VA
authors: Joshi
authors: Radhika D
authors: RD
authors: Wakharkar
authors: Ramki
authors: R
authors: Iyer
authors: Ramesh G
authors: RG
authors: Kelkar
authors: Subhash P
authors: SP
authors: Chavan
authors: Sunita S
authors: SS
authors: Kunte
mesh_terms: D000935:Antifungal Agents / Q000737:chemistry* / Q000494:pharmacology; D052160:Benzothiazoles / Q000737:chemistry*; D048588:Benzoxazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D001583:Benzoxazoles / Q000737:chemistry*; D002175:Candida / Q000187:drug effects; D015725:Fluconazole / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship; D013843:Thiazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D000935:Antifungal Agents; D052160:Benzothiazoles; D048588:Benzoxazines; D001583:Benzoxazoles; D013843:Thiazines; D015725:Fluconazole