Discovery of 5-aryloxy-2,4-thiazolidinediones as potent GPR40 agonists.

Merck Research Laboratories, Rahway, NJ 07065, USA.
Bioorganic & medicinal chemistry letters (Impact Factor: 2.65). 02/2010; 20(3):1298-301. DOI: 10.1016/j.bmcl.2009.10.052
Source: PubMed

ABSTRACT Systematic structure-activity relationship (SAR) studies of a screening lead led to the discovery of a series of thiazolidinediones (TZDs) as potent GPR40 agonists. Among them, compound C demonstrated an acute mechanism-based glucose-lowering in an intraperitoneal glucose tolerance test (IPGTT) in lean mice, while no effects were observed in GPR40 knock-out mice.

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