Lead optimization of a pyridine-carboxamide series as DGAT-1 inhibitors

  • Bioorg Med Chem Lett. 2013 Feb 15;23(4):985-8. doi: 10.1016/j.bmcl.2012.12.040.
Pauline C Ting  1 ,  Joe F Lee ,  Nicolas Zorn ,  Hyunjin M Kim ,  Robert G Aslanian ,  Mingxiang Lin ,  Michelle Smith ,  Scott S Walker ,  John Cook ,  Margaret Van Heek ,  Jean Lachowicz
Affiliations
  • 1. Department of Chemical Research, Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA. [email protected]
PMID: 23317570 DOI: 10.1016/j.bmcl.2012.12.040
Abstract

The structure-activity relationship studies of a novel series of carboxylic acid derivatives of pyridine-carboxamides as DGAT-1 inhibitors is described. The optimization of the initial lead compound 6 based on in vitro and in vivo activity led to the discovery of key compounds 10j and 17h.