Design, synthesis and SAR of a novel series of heterocyclic phenylpropanoic acids as GPR120 agonists

  • Bioorg Med Chem Lett. 2017 Aug 1;27(15):3272-3278. doi: 10.1016/j.bmcl.2017.06.028.
Xuqing Zhang  1 ,  Chaozhong Cai  2 ,  Michael Winters  2 ,  Michele Wells  2 ,  Mark Wall  2 ,  James Lanter  2 ,  Zhihua Sui  2 ,  Jingyuan Ma  3 ,  Aaron Novack  3 ,  Imad Nashashibi  3 ,  Yuanping Wang  2 ,  Wen Yan  2 ,  Arthur Suckow  2 ,  Hong Hua  2 ,  Austin Bell  2 ,  Peter Haug  2 ,  Wilma Clapper  2 ,  Celia Jenkinson  2 ,  Joseph Gunnet  2 ,  James Leonard  2 ,  William V Murray  2
Affiliations
  • 1. Cardiovascular and Metabolic Research, Janssen Research & Development, LLC, Welsh & McKean Roads, Box 776, Spring House, PA 19477, United States. Electronic address: [email protected].
  • 2. Cardiovascular and Metabolic Research, Janssen Research & Development, LLC, Welsh & McKean Roads, Box 776, Spring House, PA 19477, United States.
  • 3. CymaBay Therapeutics, Inc., 7999 Gateway Blvd, Newark, CA 94560, United States.
PMID: 28642104 DOI: 10.1016/j.bmcl.2017.06.028
Abstract

A novel series of 5-membered heterocycle-containing phenylpropanoic acid derivatives was discovered as potent GPR120 agonists with low clearance, high oral bioavailability and in vivo antidiabetic activity in rodents.

Keywords
GPR120; Phenylpropanoic acid; Type 2 diabetes.
Products