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Bioorg Med Chem Lett. 2013 May 15;23(10):2920-4. doi: 10.1016/j.bmcl.2013.03.060. Epub 2013 Mar 26.

Discovery of novel orally bioavailable GPR40 agonists.

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  • 1Shanghai Hengrui Pharmaceutical Co. Ltd, 279 Wenjing Rd., Shanghai 200245, China. lvhj@shhrp.com


The GPR40 (FFA1) has emerged as an attractive target for a novel insulin secretagogue with glucose dependency. A series of novel orally bioavailable GPR40 agonists was discovered. SAR study and structural optimization led to identification of compounds 28a and 30a as potent GPR40 agonists with superior physiochemical properties and robust in vivo efficacy in rhesus monkeys.

Copyright © 2013 Elsevier Ltd. All rights reserved.

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