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

Bioorganic & Medicinal Chemistry Letters
2010.0

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.

Knowledge Graph

Similar Paper

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
Bioorganic & Medicinal Chemistry Letters 2010.0
Synthesis and antifungal activity of 1,2,3-triazole containing fluconazole analogues
Bioorganic & Medicinal Chemistry Letters 2009.0
Design, synthesis and antifungal evaluation of 1-(2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl)-1H-1,2,4-triazol-5(4H)-one
European Journal of Medicinal Chemistry 2011.0
Synthesis and antifungal activities of new fluconazole analogues with azaheterocycle moiety
Bioorganic & Medicinal Chemistry Letters 2007.0
Novel hybrids of fluconazole and furanones: Design, synthesis and antifungal activity
Bioorganic & Medicinal Chemistry Letters 2011.0
Design, synthesis, and biological evaluation of novel 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted benzylamino-2-propanols
Bioorganic & Medicinal Chemistry Letters 2009.0
Synthesis, in vitro antifungal activity and in silico study of 3-(1,2,4-triazol-1-yl)flavanones
European Journal of Medicinal Chemistry 2013.0
Design, synthesis, and structure-activity relationship studies of benzothiazole derivatives as antifungal agents
European Journal of Medicinal Chemistry 2016.0
Synthesis and antifungal activity of 1,5-disubstituted-1,2,3-triazole containing fluconazole analogues
MedChemComm 2012.0
Synthesis and antifungal activity of some s-mercaptotriazolobenzothiazolyl amino acid derivatives
European Journal of Medicinal Chemistry 2013.0