| Literature DB >> 11720854 |
K G Liu1, M H Lambert, A H Ayscue, B R Henke, L M Leesnitzer, W R Oliver, K D Plunket, H E Xu, D D Sternbach, T M Willson.
Abstract
A series of PPARgamma agonists were synthesized from L-tyrosine that incorporated low molecular weight N-substituents. The most potent analogue, pyrrole (4e), demonstrated a K(i) of 6.9nM and an EC(50) of 4.7nM in PPARgamma binding and functional assays, respectively. Pyrrole (4e), which is readily synthesized from L-tyrosine methyl ester in four steps, also demonstrated in vivo activity in a rodent model of Type 2 diabetes.Entities:
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Year: 2001 PMID： 11720854 DOI： 10.1016/s0960-894x(01)00649-7
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823