Structure–activity relationships of 3, 5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy

…, R Yoshimoto, H Hosaka, T Hasegawa, M Chiba…

文献索引：Iino, Tomoharu; Hashimoto, Noriaki; Sasaki, Kaori; Ohyama, Sumika; Yoshimoto, Riki; Hosaka, Hideka; Hasegawa, Takuro; Chiba, Masato; Nagata, Yasufumi; Eiki, Jun-ichi; Nishimura, Teruyuki Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 11 p. 3800 - 3809

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被引用次数: 31

摘要

The optimization of our lead GK activator 2a to 3-[(1S)-2-hydroxy-1-methylethoxy]-5-[4- (methylsulfonyl) phenoxy]-N-1, 3-thiazol-2-ylbenzamide (6g), a potent GK activator with good oral availability, is described, including to uncouple the relationship between potency and hydrophobicity. Following oral administration, this compound exhibited robust glucose lowering in diabetic model rodents.