title: N-carbamoyl analogs of Zafirlukast: potent receptor antagonists of leukotriene D4.
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.
authors.affiliation: Pfizer Central Research, Groton, CT 06340, USA.
authors.forename: M F
authors.initials: MF
authors.lastname: Brown
authors.forename: A
authors.initials: A
authors.lastname: Marfat
authors.forename: G
authors.initials: G
authors.lastname: Antognoli
authors.forename: R J
authors.initials: RJ
authors.lastname: Chambers
authors.forename: J B
authors.initials: JB
authors.lastname: Cheng
authors.forename: D B
authors.initials: DB
authors.lastname: Damon
authors.forename: T E
authors.initials: TE
authors.lastname: Liston
authors.forename: M A
authors.initials: MA
authors.lastname: McGlynn
authors.forename: S P
authors.initials: SP
authors.lastname: O'Sullivan
authors.forename: B S
authors.initials: BS
authors.lastname: Owens
authors.forename: J S
authors.initials: JS
authors.lastname: Pillar
authors.forename: J T
authors.initials: JT
authors.lastname: Shirley
authors.forename: J W
authors.initials: JW
authors.lastname: Watson
mesh_terms: D000818:Animals; D006168:Guinea Pigs; D000882:Haplorhini; D006801:Humans; D007211:Indoles; D020024:Leukotriene Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology*; D008565:Membrane Proteins; D008956:Models, Chemical; D048448:Phenylcarbamates; D051381:Rats; D018077:Receptors, Leukotriene; D013449:Sulfonamides; D014105:Tosyl Compounds / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D007211:Indoles; D020024:Leukotriene Antagonists; D008565:Membrane Proteins; D048448:Phenylcarbamates; D018077:Receptors, Leukotriene; D013449:Sulfonamides; D014105:Tosyl Compounds; C412375:cysteinyl leukotriene receptor 2; C083169:leukotriene D4 receptor; C062735:zafirlukast