GPR119 is a G-protein-coupled receptor mainly expressed in pancreatic islets and gastrointestinal tract. Activation of the GPR119 receptor stimulates glucose-dependent insulin secretion from �-cells and GLP1 secretion from the L-cells. Thus, agonists of GPR119 are promising oral glucose lowering agents for type II diabetes. Here we report the discovery of a novel class of benzothiazole analogs as potent GPR119 agonists. The synthesis, structure-activity relationship (SAR) studies and the in vivo preclinical pharmacology will be discussed.                                                      

Discovery of novel benzothiazole derivatives as potent GPR119 agonists for the treatment of type II diabetes

244th National Meeting (2012)

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