N-carbamoyl analogs of Zafirlukast: potent receptor antagonists of leukotriene D4

  • Bioorg Med Chem Lett. 1998 Sep 22;8(18):2451-6. doi: 10.1016/s0960-894x(98)00442-9.
M F Brown  1 ,  A Marfat ,  G Antognoli ,  R J Chambers ,  J B Cheng ,  D B Damon ,  T E Liston ,  M A McGlynn ,  S P O'Sullivan ,  B S Owens ,  J S Pillar ,  J T Shirley ,  J W Watson
Affiliations
  • 1. Pfizer Central Research, Groton, CT 06340, USA.
PMID: 9873560 DOI: 10.1016/s0960-894x(98)00442-9
Abstract

Exploration of the indole nitrogen region of Zafirlukast (1) has uncovered a potent series of cysteinyl leukotriene D4 (LTD4) antagonists. These studies showed that a variety of functionality could be incorporated in this region of the molecule without sacrificing potency. Efforts to exploit this site in order to improve oral efficacy are discussed.