Discovery of 317318-97-1

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Synthetic Route of 317318-97-1. Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments.Introducing a new discovery about 317318-97-1, Name is 5-(Chloromethyl)-4-methyl-2-(4-(trifluoromethyl)phenyl)thiazole

Optimization of GPR40 agonists for type 2 diabetes

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 hemoglobin A1c (HbA1c) and lowered both postprandial and fasting blood glucose levels in type 2 diabetic patients in phase II clinical trials. We optimized phenylpropanoic acid derivatives as GPR40 agonists and identified AMG 837 (2) as a clinical 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 minimum central nervous system (CNS) penetration.

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Reference:
Thiazole | C3H6007NS – PubChem,
Thiazole | chemical compound | Britannica