2. Academic Validation
  3. Design, synthesis and SAR of a novel series of heterocyclic phenylpropanoic acids as GPR120 agonists

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

Affiliations

  • 1 Cardiovascular and Metabolic Research, Janssen Research & Development, LLC, Welsh & McKean Roads, Box 776, Spring House, PA 19477, United States. Electronic address: xzhang5@its.jnj.com.
  • 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.

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