针对质膜H[+]- atp酶的新型抗真菌药物的合成与评价

D. Patel, J. Bassin, D. G. Griffiths
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引用次数: 1

摘要

合成了一系列二烯酮类候选抗真菌药物。这些化合物对酿酒酵母菌和白色念珠菌进行了药敏试验。二烯酮对酿酒葡萄球菌(0.2 ~ 99%)和白色念珠菌(0 ~ 99%)的抑制范围较广。3,5-二(对三氟甲基苄基)-1-甲基哌啶-4- 1被鉴定为最有效的酿酒葡萄球菌抑制剂。而最有希望的白色念珠菌抑制剂是2,6-二(吡啶-3基亚甲基)环己烷-1- 1。
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Synthesis and evaluation of novel antifungal agents targeted to the plasma membrane H[+]-ATPase
A library of dienones were synthesized as candidate antifungal agents. These compounds were screened against Saccharomyces cerevisiae and Candida albicans using macro-broth susceptibility assay. The dienones exhibited a broad range of inhibition against S. cerevisiae (0.2-99%) and C. albicans (0-99%). 3,5-bis(p- trifluoromethylbenzylidene)-1-methyl-piperidine-4-one was identified as the most potent inhibitor of S. cerevisiae. Whereas, the most promising inhibitor of C. albicans was 2,6-bis(pyridine-3ylmethylene)cyclohexan-1-one.
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