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Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene D4 receptor antagonists. 4. Addition of chromone moiety enhances leukotriene D4 receptor binding affinity
Journal of Medicinal Chemistry1991Vol. 34(5), pp. 1704–1707
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Fu Chih Huang, Robert A. Galemmo, Gregory Poli, Keith S. Learn, Mathew M. Morrissette, William H. Johnson, William P. Dankulich, H. F. Campbell, Gilbert W. Carnathan, Richard G. Van Inwegen
Abstract
The combination of the benzopyran-4-one ring, a moiety found in the prototype leukotriene antagonist, FPL 55,712, with the (2-quinolinylmethoxy)phenyl group led to a significant increase in leukotriene receptor binding affinity. This modification resulted in a 10,000-fold improvement in binding affinity compared to FPL 55,712. Compound 7 (RG 12553), with a Ki value of 0.1 nM, has higher affinity than the natural agonist LTD4 and is one of the most potent LTD4 antagonists reported. The structure-activity relationships of this series of potent leukotriene antagonists are discussed.
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