- Design and optimization of highly-selective fungal CYP51 inhibitors
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While the orally-active azoles such as voriconazole and itraconazole are effective antifungal agents, they potently inhibit a broad range of off-target human cytochrome P450 enzymes (CYPs) leading to various safety issues (e.g., drug-drug interactions, li
- Hoekstra, William J.,Garvey, Edward P.,Moore, William R.,Rafferty, Stephen W.,Yates, Christopher M.,Schotzinger, Robert J.
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p. 3455 - 3458
(2014/07/22)
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- METALLOENZYME INHIBITOR COMPOUNDS
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The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
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Page/Page column 116-119
(2013/02/28)
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- New antifungal 1,2,4-triazoles with difluoro(heteroaryl)methyl moiety
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New 1,2,4-triazoles (1) having a difluoro(heteroaryl)methyl moiety were designed and synthesized via 1-aryl-2,2-difluoro-2- (heteroaryl)ethanones (2), which were prepared by two routes starting from the reaction of ethyl 2,2- difluoro(heteroaryl)acetate with phenyllithiums (Route A) and from the reaction of chlorodifluoro(heteroaryl)methane with benzaldehydes (Route B). The compounds 1 except for 1g show antifungal activities against yeasts and filamentous fungi in vitro, especially (+)-If have equal or superior activities compared to those of itraconazole.
- Eto, Hiromichi,Kaneko, Yasushi,Sakamoto, Takao
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p. 982 - 990
(2007/10/03)
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