Substituted coumarins as potent 5-lipoxygenase inhibitors.
Leukotriene biosynthesis inhibitors have potential as therapeutic agents for asthma and inflammatory diseases. A novel series of substituted coumarin derivatives has been synthesized and the structure-activity relationship was evaluated with respect to their ability to inhibit the formation of leukotrienes via the human 5-lipoxygenase enzyme.
Grimm
Erich L
EL
Merck Frosst Centre for Therapeutic Research, 16711 Trans Canada Hwy, Kirkland, Que., Canada H9H 3L1. erich_grimm@merck.com
Brideau
Christine
C
Chauret
Nathalie
N
Chan
Chi-Chung
CC
Delorme
Daniel
D
Ducharme
Yves
Y
Ethier
Diane
D
Falgueyret
Jean-Pierre
JP
Friesen
Richard W
RW
Guay
Jocelyne
J
Hamel
Pierre
P
Riendeau
Denis
D
Soucy-Breau
Chantal
C
Tagari
Philip
P
Girard
Yves
Y
D003374:Coumarins / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D016859:Lipoxygenase Inhibitors; D015394:Molecular Structure; D013329:Structure-Activity Relationship
D003374:Coumarins; D004791:Enzyme Inhibitors; D016859:Lipoxygenase Inhibitors