2. Academic Validation
  3. Discovery of pyrazolyl propionyl cyclohexenamide derivatives as full agonists for the high affinity niacin receptor GPR109A

Discovery of pyrazolyl propionyl cyclohexenamide derivatives as full agonists for the high affinity niacin receptor GPR109A

  • Bioorg Med Chem Lett. 2010 Jun 1;20(11):3372-5. doi: 10.1016/j.bmcl.2010.04.013.
Fa-Xiang Ding 1,  Hong C Shen,  Larrisa C Wilsie,  Mihajlo L Krsmanovic,  Andrew K Taggart,  Ning Ren,  Tian-Quan Cai,  Junying Wang,  Xinchun Tong,  Tom G Holt,  Qing Chen,  M Gerard Waters,  Milton L Hammond,  James R Tata,  Steven L Colletti
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065-0900, USA. [email protected]
PMID: 20452209 DOI: 10.1016/j.bmcl.2010.04.013
Abstract

A series of pyrazolyl propionyl cyclohexenamides were discovered as full agonists for the high affinity niacin receptor GPR109A. The structure-activity relationship (SAR) studies were aimed to improve activity on GPR109A, reduce Cytochrome P450 2C8 (CYP2C8) and Cytochrome P450 2C9 (CYP2C9) inhibition, reduce serum shift and improve pharmacokinetic (PK) profiles.

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