Structure-activity relationships of 1,3-benzoxazole-4-carbonitriles as novel antifungal agents with potent in vivo efficacy |
| |
| Authors: | Kuroyanagi Jun-ichi Kanai Kazuo Horiuchi Takao Takeshita Hiroshi Kobayashi Shozo Achiwa Issei Yoshida Kumi Nakamura Koichi Kawakami Katsuhiro |
| |
| Institution: | Lead Discovery & Optimization Research Laboratories II, Daiichi Sankyo Co., Ltd., Tokyo, Japan. kuroyanagi.junichi.d5@daiichisankyo.co.jp |
| |
| Abstract: | 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 16b showed potent in vivo efficacy against mice Candida infection models and good bioavailability in rats. |
| |
| Keywords: | |
| 本文献已被 PubMed 等数据库收录！ |
|
