Literature DB >> 24332491

Discovery and optimization of N-(3-(1,3-dioxo-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-4-yloxy)phenyl)benzenesulfonamides as novel GPR119 agonists.

Ming Yu1, Jian Ken Zhang2, Yingcai Wang2, Jiang Zhu2, Frank Kayser2, Julio C Medina2, Karen Siegler3, Marion Conn3, Bei Shan3, Mark P Grillo4, Peter Coward3, Jiwen Jim Liu2.   

Abstract

The discovery and optimization of novel N-(3-(1,3-dioxo-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-4-yloxy)phenyl)benzenesulfonamide GPR119 agonists is described. Modification of the pyridylphthalimide motif of the molecule with R(1)=-Me and R(2)=-(i)Pr substituents, incorporated with a 6-fluoro substitution on the central phenyl ring offered a potent and metabolically stable tool compound 22.
Copyright © 2013 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Agonist; GPR119; Type 2 diabetes

Mesh:

Substances:

Year:  2013        PMID: 24332491     DOI: 10.1016/j.bmcl.2013.11.053

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


  1 in total

Review 1.  An Overview of the Biological Activity of Pyrrolo[3,4-c]pyridine Derivatives.

Authors:  Anna Wójcicka; Aleksandra Redzicka
Journal:  Pharmaceuticals (Basel)       Date:  2021-04-11
  1 in total

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