Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy.
Basic Information
ID: ALA1151922
Journal: Bioorg Med Chem
Title: Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy.
Authors: Iino T, Hashimoto N, Sasaki K, Ohyama S, Yoshimoto R, Hosaka H, Hasegawa T, Chiba M, Nagata Y, Eiki J, Nishimura T.
Abstract: 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.
CiteXplore: 19427223
DOI: 10.1016/j.bmc.2009.04.040
Patent ID: ┄