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ID: ALA3596131

Journal: Bioorg Med Chem Lett

Title: Discovery of a novel trans-1,4-dioxycyclohexane GPR119 agonist series.

Authors: Han S, Narayanan S, Kim SH, Calderon I, Zhu X, Kawasaki A, Yue D, Lehmann J, Wong A, Buzard DJ, Semple G, Carroll C, Chu ZL, Al-Sharmma H, Shu HH, Tung SF, Unett DJ, Behan DP, Yoon WH, Morgan M, Usmani KA, Chen C, Sadeque A, Leonard JN, Jones RM.

Abstract: The design and optimization of a novel trans-1,4-dioxycyclohexane GPR119 agonist series is described. A lead compound 21 was found to be a potent and efficacious GPR119 agonist across species, and possessed overall favorable pharmaceutical properties. Compound 21 demonstrated robust acute and chronic regulatory effects on glycemic parameters in the diabetic or non-diabetic rodent models.

CiteXplore: 26048791

DOI: 10.1016/j.bmcl.2015.04.102