Development of new chromanol antagonists of leukotriene D4.
By addressing the issues of potency and metabolism in 3, a new series of LTD4 antagonists represented by (+)-26 was developed which is equipotent to clinical LTD4 antagonists Zafirlukast (1) and Pranlukast (2).
Chambers
R J
RJ
Central Research Division, Pfizer Inc., Groton, CT 06340, USA.
Antognoli
G W
GW
Cheng
J B
JB
Marfat
A
A
Pillar
J S
JS
Shirley
J T
JT
Watson
J W
JW
D000818:Animals; D002839:Chromans / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D002867:Chromones / Q000494:pharmacology; D006168:Guinea Pigs; D006801:Humans; D007211:Indoles; D020024:Leukotriene Antagonists / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D017998:Leukotriene D4 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D048448:Phenylcarbamates; D011485:Protein Binding; D013449:Sulfonamides; D014105:Tosyl Compounds / Q000494:pharmacology
D002839:Chromans; D002867:Chromones; D007211:Indoles; D020024:Leukotriene Antagonists; D048448:Phenylcarbamates; D013449:Sulfonamides; D014105:Tosyl Compounds; D017998:Leukotriene D4; C029141:2,2,5,7,8-pentamethyl-1-hydroxychroman; C047681:pranlukast; C062735:zafirlukast