Discovery of potent and orally active 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as novel allosteric glucokinase activators

…, D Tsukahara, K Kamata, K Sasaki, S Ohyama…

文献索引：Iino, Tomoharu; Tsukahara, Daisuke; Kamata, Kenji; Sasaki, Kaori; Ohyama, Sumika; Hosaka, Hideka; Hasegawa, Takuro; Chiba, Masato; Nagata, Yasufumi; Eiki, Jun-ichi; Nishimura, Teruyuki Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 7 p. 2733 - 2743

全文：HTML全文

被引用次数: 30

摘要

Identification and synthesis of novel 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as glucokinase activators are described. Removal of an aniline structure of the prototype lead (2a) and incorporation of an alkoxy or phenoxy substituent led to the identification of 3- Isopropoxy-5-[4-(methylsulfonyl) phenoxy]-N-(4-methyl-1, 3-thiazol-2-yl) benzamide (27e) as a novel, potent, and orally bioavailable GK activator. Rat oral glucose tolerance test ...