Discovery of N-arylpyrroles as agonists of GPR120 for the treatment of type II diabetes. Issue 5 (1st March 2018)

• Record Type: Journal Article
• Authors: Winters, Michael P.; Sui, Zhihua; Wall, Mark; Wang, Yuanping; Gunnet, Joseph; Leonard, James; Hua, Hong; Yan, Wen; Suckow, Arthur; Bell, Austin; Clapper, Wilmelenne; Jenkinson, Celia; Haug, Peter; Koudriakova, Tatiana; Huebert, Norman; Murray, William V.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 28:Issue 5(2018)
• Page Start: 841
• Page End: 846
• Publication Date: 2018-03-01
• Subjects: GPR120 -- FFAR4 -- N-arylpyrrole -- Type 2 diabetes -- GPR40 -- oGTT -- DIO mouse; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2018.02.013
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: The discovery of a novel series of N -arylpyrroles as agonists of GPR120 (FFAR4) is discussed. Compound27 is a potent GPR120 agonist, has good selectivity for related receptor GPR40 (FFAR1), has acceptable PK properties, and is active in 2 models of Type 2 Diabetes in mice. Abstract: The discovery of a novel series of N -arylpyrroles as agonists of GPR120 (FFAR4) is discussed. One lead compound is a potent GPR120 agonist, has good selectivity for related receptor GPR40 (FFAR1), has acceptable PK properties, and is active in 2 models of Type 2 Diabetes in mice.