Format

Send to

Choose Destination
Bioorg Med Chem Lett. 2007 Mar 15;17(6):1584-9. Epub 2007 Jan 4.

Solid phase synthesis and SAR of small molecule agonists for the GPR40 receptor.

Author information

1
Molecular Discovery Research, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. Steve.C.McKeown@gsk.com

Abstract

The discovery, synthesis and structure-activity relationship (SAR) of novel carboxylic acid agonists for GPR40 are described. Aryl propionic acid 1, identified from a high throughput screen, was selected for chemical exploration. Compound 2 was identified as our lead molecule through efficient solid phase combinatorial array chemistry and had an attractive in vitro and in vivo pharmacokinetic profile in rat. These ligands may prove useful in establishing a role for GPR40 in insulin regulation.

PMID:
17240142
DOI:
10.1016/j.bmcl.2006.12.084
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center