TY - JOUR T1 - Novel hybrids of fluconazole and furanones: design, synthesis and antifungal activity JF - Bioorganic & Medicinal Chemistry Letters Y1 - 2011 A1 - Borate, Hanumant B. A1 - Sawargave, Sangmeshwer P. A1 - Chavan, Subhash P. A1 - Chandavarkar, Mohan A. A1 - Iyer, Ramki A1 - Tawte, Amit A1 - Rao, Deepali A1 - Deore, Jaydeep V. A1 - Kudale, Ananada S. A1 - Mahajan, Pankaj S. A1 - Kangire, Gopinath S. KW - Antifungal activity KW - Fluconazole KW - Furanones AB -

During our efforts to develop new antifungal agents, a number of hybrid molecules containing furanones and fluconazole pharmacophores were designed and synthesized. The new chemical entities thus synthesized were tested for their potential as antifungal agents against various fungal strains and it was observed that the compounds with general structure 7 were potent inhibitors of Candida albicans ATCC 24433, Candida glabrata ATCC 90030, Candida tropicalis ATCC 750 and Candida neoformans ATCC 34664 while the fluconazole analogues 12 exhibited antifungal activity against Candida albicans ATCC 24433 and Candida glabrata ATCC 90030. The structure-activity relationship for these compounds is discussed. The synthetic strategies used in the present work have potential to prepare a large number of compounds for further refinement of structures to obtain molecules suitable for development as antifungal drugs. (C) 2011 Elsevier Ltd. All rights reserved.

PB - PERGAMON-ELSEVIER SCIENCE LTD CY - THE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLAND VL - 21 IS - 16 U3 - 3.00 U4 - 3.00 ER -