Literature DB >> 23648181

Discovery and optimization of arylsulfonyl 3-(pyridin-2-yloxy)anilines as novel GPR119 agonists.

Jian Ken Zhang1, An-Rong Li, Ming Yu, Yingcai Wang, Jiang Zhu, Frank Kayser, Julio C Medina, Karen Siegler, Marion Conn, Bei Shan, Mark P Grillo, John Eksterowicz, Peter Coward, Jiwen Jim Liu.   

Abstract

We describe the discovery of a series of arylsulfonyl 3-(pyridin-2-yloxy)anilines as GPR119 agonists derived from compound 1. Replacement of the three methyl groups in 1 with metabolically stable moieties led to the identification of compound 34, a potent and efficacious GPR119 agonist with improved pharmacokinetic (PK) properties.
Copyright © 2013 Elsevier Ltd. All rights reserved.

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Year:  2013        PMID: 23648181     DOI: 10.1016/j.bmcl.2013.04.014

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Identification of Novel, Structurally Diverse, Small Molecule Modulators of GPR119.

Authors:  Ainhoa Nieto; Virneliz Fernández-Vega; Timothy P Spicer; Emmanuel Sturchler; Pramisha Adhikari; Nicole Kennedy; Sean Mandat; Peter Chase; Louis Scampavia; Thomas Bannister; Peter Hodder; Patricia H McDonald
Journal:  Assay Drug Dev Technol       Date:  2018-07       Impact factor: 1.738

2.  Discovery of 5-methyl-2-(4-((4-(methylsulfonyl)benzyl)oxy)phenyl)-4-(piperazin-1-yl)pyrimidine derivatives as novel GRP119 agonists for the treatment of diabetes and obesity.

Authors:  Jinying Chen; Zitai Sang; Lu Li; Linhong He; Liang Ma
Journal:  Mol Divers       Date:  2017-06-27       Impact factor: 2.943

  2 in total

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