A new class of leukotriene biosynthesis inhibitors: The discovery of MK0591

The evolution of a quinoline based FLAP inhibitor, L-674,636, into a novel quinoline-indole hybrid compound: MK0591, is described. The new series of compounds are more potent, particularly in binding to FLAP, in inhibiting LTB 4 biosynthesis in stimulated human PMN, and in the human whole blood assa...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1992-11, Vol.2 (11), p.1395-1398
Main Authors: Prasit, P., Belley, M., Brideau, C., Chan, C., Charleson, S., Evans, J.F., Fortin, R., Ford-Hutchinson, A.W., Gillard, J.W., Guay, J., Hutchinson, J.H., Léger, S., Riendeau, D., Young, R.N., Zamboni, R.
Format: Article
Language:English
Subjects:
Chemistry
Chemistry, Medicinal
Chemistry, Organic
Life Sciences & Biomedicine
Pharmacology & Pharmacy
Physical Sciences
Science & Technology
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Summary:The evolution of a quinoline based FLAP inhibitor, L-674,636, into a novel quinoline-indole hybrid compound: MK0591, is described. The new series of compounds are more potent, particularly in binding to FLAP, in inhibiting LTB 4 biosynthesis in stimulated human PMN, and in the human whole blood assay.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(00)80520-X