Three 3-(halogenated phenyl)-5-acyloxymethyl-2,5-dihydrofuran-2-ones were evaluated for activity against 191 strains of common and emerging yeasts and Aspergillus species by the broth microdilution test performed according to NCCLS guidelines. The furanone derivatives displayed broad-spectrum in vitro activity against potentially pathogenic yeasts and molds, especially Aspergillus spp. (MIC

• MeSH
• Antifungal Agents pharmacology   toxicity   MeSH
• Fluconazole pharmacology   MeSH
• Drug Resistance, Fungal MeSH
• Furans pharmacology   toxicity   MeSH
• Fungi drug effects   ultrastructure   MeSH
• Yeasts drug effects   ultrastructure   MeSH
• Lethal Dose 50 MeSH
• Leukemia L1210 drug therapy   MeSH
• Humans MeSH
• Microbial Sensitivity Tests MeSH
• Mycoses microbiology   MeSH
• Mice MeSH
• Antineoplastic Agents pharmacology   MeSH
• Animals MeSH
• Check Tag
• Humans MeSH
• Male MeSH
• Mice MeSH
• Animals MeSH
• Publication type
• Journal Article MeSH
• Research Support, Non-U.S. Gov't MeSH
• Names of Substances
• Antifungal Agents MeSH
• Fluconazole MeSH
• Furans MeSH
• Antineoplastic Agents MeSH

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.

• MeSH
• Antifungal Agents pharmacology   MeSH
• Fungi drug effects   MeSH
• Humans MeSH
• Microbial Sensitivity Tests MeSH
• Oxazines chemical synthesis   chemistry   pharmacology   MeSH
• Spectrophotometry, Infrared MeSH
• Structure-Activity Relationship MeSH
• Check Tag
• Humans MeSH
• Publication type
• Journal Article MeSH
• Research Support, Non-U.S. Gov't MeSH
• Names of Substances
• Antifungal Agents MeSH
• Oxazines MeSH