1. Academic Validation
  2. Lead optimization of a pyridine-carboxamide series as DGAT-1 inhibitors

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

Affiliation

  • 1 Department of Chemical Research, Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA. pauline.ting@merck.com
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.

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