Liu, Jiwen published the artcileOptimization of GPR40 Agonists for Type 2 Diabetes, Recommanded Product: 4-Chloro-2-methylphenylboronic acid, the publication is ACS Medicinal Chemistry Letters (2014), 5(5), 517-521, database is CAplus and MEDLINE.
GPR40 (FFA1 and FFAR1) has gained significant interest as a target for the treatment of type 2 diabetes. TAK-875 (1), a GPR40 agonist, lowered Hb A1c (HbA1c) and lowered both postprandial and fasting blood glucose levels in type 2 diabetic patients in phase II clin. trials. We optimized phenylpropanoic acid derivatives as GPR40 agonists and identified AMG 837 (2) as a clin. candidate. Here we report our efforts in searching for structurally distinct back-ups for AMG 837. These efforts led to the identification of more polar GPR40 agonists, such as AM-4668 (10), that have improved potency, excellent pharmacokinetic properties across species, and min. central nervous system (CNS) penetration.
ACS Medicinal Chemistry Letters published new progress about 209919-30-2. 209919-30-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is 4-Chloro-2-methylphenylboronic acid, and the molecular formula is C7H8BClO2, Recommanded Product: 4-Chloro-2-methylphenylboronic acid.
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