title: A series of non-quinoline cysLT1 receptor antagonists: SAR study on pyridyl analogs of Singulair.
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.
authors.affiliation: Merck Frosst Center for Therapeutic Research, Québec, Canada.
authors.forename: D
authors.initials: D
authors.lastname: Guay
authors.forename: J Y
authors.initials: JY
authors.lastname: Gauthier
authors.forename: C
authors.initials: C
authors.lastname: Dufresne
authors.forename: T R
authors.initials: TR
authors.lastname: Jones
authors.forename: M
authors.initials: M
authors.lastname: McAuliffe
authors.forename: C
authors.initials: C
authors.lastname: McFarlane
authors.forename: K M
authors.initials: KM
authors.lastname: Metters
authors.forename: P
authors.initials: P
authors.lastname: Prasit
authors.forename: C
authors.initials: C
authors.lastname: Rochette
authors.forename: P
authors.initials: P
authors.lastname: Roy
authors.forename: N
authors.initials: N
authors.lastname: Sawyer
authors.forename: R
authors.initials: R
authors.lastname: Zamboni
mesh_terms: D000085:Acetates / Q000737:chemistry* / Q000494:pharmacology*; D000818:Animals; D018927:Anti-Asthmatic Agents / Q000737:chemistry / Q000494:pharmacology*; D003521:Cyclopropanes; D006168:Guinea Pigs; D006801:Humans; D020024:Leukotriene Antagonists / Q000737:chemistry / Q000494:pharmacology*; D008565:Membrane Proteins; D011725:Pyridines / Q000737:chemistry / Q000494:pharmacology; D011804:Quinolines / Q000737:chemistry* / Q000494:pharmacology*; D051381:Rats; D018077:Receptors, Leukotriene; D012453:Saimiri; D013329:Structure-Activity Relationship; D013440:Sulfides
chemical_list: D000085:Acetates; D018927:Anti-Asthmatic Agents; D003521:Cyclopropanes; C116447:L 733321; D020024:Leukotriene Antagonists; D008565:Membrane Proteins; D011725:Pyridines; D011804:Quinolines; D018077:Receptors, Leukotriene; D013440:Sulfides; C412375:cysteinyl leukotriene receptor 2; C083169:leukotriene D4 receptor; C093875:montelukast