Structure-Activity Relationships of 1, 3-Benzoxazole-4-carbonitriles as Novel Antifungal Agents with Potent in Vivo Efficacy

J Kuroyanagi, K Kanai, T Horiuchi, H Takeshita…

文献索引：Kuroyanagi, Jun-Ichi; Kanai, Kazuo; Horiuchi, Takao; Takeshita, Hiroshi; Kobayashi, Shozo; Achiwa, Issei; Yoshida, Kumi; Nakamura, Koichi; Kawakami, Katsuhiro Chemical and Pharmaceutical Bulletin, 2011 , vol. 59, # 3 p. 341 - 352

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被引用次数: 6

摘要

A series of 1, 3-benzoxazole-4-carbonitriles was synthesized and evaluated for its antifungal activity, solubility, and metabolic stability. Among those compounds, 4-cyano-N, N, 5- trimethyl-7-[(3S)-3-methyl-3-(methylamino) pyrrolidin-1-yl]-6-phenyl-1, 3-benzoxazole-2- carboxamide (16b) exhibited potent in vitro activity against Candida species, higher water solubility, and improved metabolic stability compared to lead compound 1. Compound ...