A series of non-quinoline cysLT1 receptor antagonists: SAR study on pyridyl analogs of Singulair

  • Bioorg Med Chem Lett. 1998 Mar 3;8(5):453-8. doi: 10.1016/s0960-894x(98)00051-1.
D Guay  1 ,  J Y Gauthier ,  C Dufresne ,  T R Jones ,  M McAuliffe ,  C McFarlane ,  K M Metters ,  P Prasit ,  C Rochette ,  P Roy ,  N Sawyer ,  R Zamboni
Affiliations
  • 1. Merck Frosst Center for Therapeutic Research, Québec, Canada.
PMID: 9871597 DOI: 10.1016/s0960-894x(98)00051-1
Abstract

The structure-activity relationship of a series of styrylpyridine analogs of MK-0476 (montelukast, Singulair) is described. This work has led to the identification of a number of potent and orally active cysLT1 receptor (LTD4 receptor) antagonists including 2ab (L-733,321) as an optimized candidate.