In vitro antifungal activity of 3-phenyl-2H-benzoxazine-2,4(3H)-diones
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Updated: Sep 28, 2026

Broth Microdilution In Vitro Screening: An Easy and Fast Method to Detect New Antifungal Compounds
Published on: February 14, 2018
K Waisser1, L Kubicová, V Buchta
1Department of Inorganic and Organic Chemistry, Charles University, Faculty of Pharmacy, 500 05 Hradec Králové, Czechia. waisser@faf.cuni.cz
Abstract:
A series of 81 3-phenyl-2H-benzoxazine-2,4(3H)-diones with substitution at C(6) on the benzoxazine ring and on the phenyl moiety was synthesized; the compounds were evaluated for antifungal activity against five strains of potentially pathogenic fungi (Absidia corymbifera, Aspergillus fumigatus, Candida albicans, Microsporum gypseum and Trichophyton mentagrophytes). Structure-activity relationships against T. mentagrophytes and M. gypseum were determined using the Free-Wilson method, which was further combined with the approach of Hansch. In vitro antifungal activity becomes higher with increasing electron-accepting ability of the substituents on the phenyl ring, and with increasing lipophilicity.
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