126917-43-9Relevant articles and documents
Synthesis and biological evaluation of vinyl ether-containing azole derivatives as inhibitors of Trichophyton rubrum
Wang, Lulu,Yang, Wenge,Wang, Kai,Zhu, Jing,Shen, Fei,Hu, Yonghong
scheme or table, p. 4887 - 4890 (2012/08/07)
In an attempt to search for many target compounds with excellent activities, a series of vinyl ether-containing azole derivatives were designed, synthesized, and evaluated as antifungal agents. Results of preliminary antifungal tests against Trichophyton rubrum in vitro indicated that most of the synthesized compounds showed excellent activities. In comparison with fluconazole, itraconazole, voriconazole, omoconazole and amphotericin B, several compounds (such as 7d, 7g and 7h) exhibited more potent inhibitory activities, suggesting that they were promising leads for the development of novel antifungal agents.
Azole compounds as therapeutic agents for fungal infections
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Page column 32-33, (2010/02/05)
The present invention relates to the derivatives of specially substituted azole compounds which have improved antifungal activity as compared to known compounds such as fluconazole and itraconazole and the processes for the preparation thereof. This invention also relates to pharmaceutical compositions containing the compounds of the present invention and their use in treating and/or preventing fungal infections in mammals, preferably humans.
Concise Synthesis of Optically Active Oxirane Precursors for the Preparation of Triazole Antifungals Using the Friedel-Crafts Reaction of (S)-2-Tosyloxypropionyl Chloride
Konosu, Toshiyuki,Tajima, Yawara,Miyaoka, Takeo,Oida, Sadao
, p. 7545 - 7548 (2007/10/02)
Optically active epoxide (2R,3S)-4, a key intermediate for the preparation of triazole antifungal agents (4R,5R)-1 and (2R,3R)-2 (X = 2,4-F2), was synthesized.The Friedel-Crafts reaction between the (S)-lactic acid derivative (S)-10 and m-difluorobenzene gave the (R)-2-chloropropiophenone derivative (R)-11, which was converted into (2R,3R)-18 via Peterson olefination, stereoselective osmium(VIII) oxide oxidation, and mesylation.Treatment of (2R,3R)-18 with sodium triazolide gave (2R,3S)-4.Similarly, the 4-chlorophenyl analog (2R,3S)-4' was prepared.