YAKHAK HOEJI (약학회지)

The Pharmaceutical Society of Korea (대한약학회)
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Synthesis of 1,3-Dioxolan-2-yliden Derivatives and Their Antifungal Activities

1,3-Dioxolan-2-yliden 유도체들의 합성과 항진균 활성

  • Published : 1999.10.01
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Abstract

(1H-1,2,4-Triazolyl) methy-4-(sub). phenyl-5-methyl-1,3-dioxolan-2-yliden (3) derivatives were synthesized and tested for their antifungal activities. The designed compounds with a 1,2,4-triazolylmethyl group at the 4-position of 1,3-dioxolan-2-yliden moiety were synthesized by reaction of difluorinated olefins(2) with (2R, 3R)-2-(2,4-dihalophenyl)-1-(1H-1,2,4-triazol-l-yl) butane-2,3-diol (1). These compounds were tested for in vitro antifungal activities against 16 fungi species. The MIC values were determined by the micro broth dilution method. In general, 1,3-dioxolan-2-yliden derivatives showed antifungal activities in vitro. Among them, (4R, 5R)-4-(2,4-difluorophenyl)-5-methyl-2-[1-(3,4-methylenedioxypheny)meth-ylidene)-1,3-dioxolon-4-yl(1H-1,2,4-triazollyl)methane showed superior antifungal activities to fluconazol and ketoconazol.

Keywords

References

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