2. Academic Validation
  3. N-carbamoyl analogs of Zafirlukast: potent receptor antagonists of leukotriene D4

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

Affiliation

  • 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.

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