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.
MeSH terms
-
Acetates / chemistry*
-
Acetates / pharmacology*
-
Animals
-
Anti-Asthmatic Agents / chemistry
-
Anti-Asthmatic Agents / pharmacology*
-
Cyclopropanes
-
Guinea Pigs
-
Humans
-
Leukotriene Antagonists* / chemistry
-
Leukotriene Antagonists* / pharmacology*
-
Membrane Proteins*
-
Pyridines / chemistry
-
Pyridines / pharmacology
-
Quinolines / chemistry*
-
Quinolines / pharmacology*
-
Rats
-
Receptors, Leukotriene*
-
Saimiri
-
Structure-Activity Relationship
-
Sulfides
Substances
-
Acetates
-
Anti-Asthmatic Agents
-
Cyclopropanes
-
L 733321
-
Leukotriene Antagonists
-
Membrane Proteins
-
Pyridines
-
Quinolines
-
Receptors, Leukotriene
-
Sulfides
-
cysteinyl leukotriene receptor 2
-
leukotriene D4 receptor
-
montelukast