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  • Title: Discovery of potent and orally active 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as novel allosteric glucokinase activators.
    Author: Iino T, Tsukahara D, Kamata K, Sasaki K, Ohyama S, Hosaka H, Hasegawa T, Chiba M, Nagata Y, Eiki J, Nishimura T.
    Journal: Bioorg Med Chem; 2009 Apr 01; 17(7):2733-43. PubMed ID: 19282189.
    Abstract:
    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 indicated that 27e exhibited a glucose-lowering effect after 10 mg/kg oral administration.
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