A series of non-quinoline cysLT1 receptor antagonists: SAR study on pyridyl analogs of Singulair.
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.
Guay
D
D
Merck Frosst Center for Therapeutic Research, Québec, Canada.
Gauthier
J Y
JY
Dufresne
C
C
Jones
T R
TR
McAuliffe
M
M
McFarlane
C
C
Metters
K M
KM
Prasit
P
P
Rochette
C
C
Roy
P
P
Sawyer
N
N
Zamboni
R
R
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
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