4.5 Article

Discovery of the imidazole-derived GPR40 agonist AM-3189

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 26, Issue 1, Pages 15-20

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2015.11.050

Keywords

GPR40; FFAR1; GPCR; Agonist; Type II diabetes; Insulin secretagogue; AMG 837; AM-3189

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As a follow-up to the GPR40 agonist AMG 837, which was evaluated in clinical trials for the treatment of type II diabetes, further optimization led to the discovery of AM-3189 (13k). AM-3189 is representative of a new class of compounds with minimal CNS penetration, superior pharmacokinetic properties and in vivo efficacy comparable to AMG 837. (C) 2015 Elsevier Ltd. All rights reserved.

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