Discovery and optimization of a novel series of GPR142 agonists for the treatment of type 2 diabetes mellitus.
Basic Information
ID: ALA2069182
Journal: Bioorg Med Chem Lett
Title: Discovery and optimization of a novel series of GPR142 agonists for the treatment of type 2 diabetes mellitus.
Authors: Lizarzaburu M, Turcotte S, Du X, Duquette J, Fu A, Houze J, Li L, Liu J, Murakoshi M, Oda K, Okuyama R, Nara F, Reagan J, Yu M, Medina JC.
Abstract: The discovery and initial optimization of a series of phenylalanine based agonists for GPR142 is described. The structure-activity-relationship around the major areas of the molecule was explored to give agonists 90 times more potent than the initial HTS hit in a human GPR142 inositol phosphate accumulation assay. Removal of CYP inhibition by exploration of the pyridine A-ring is also described.
CiteXplore: 22884988
DOI: 10.1016/j.bmcl.2012.07.063
Patent ID: ┄