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Design, synthesis and bronchodilatory activity of a series of quinazoline-3-oxides
D W Combs1, M S Rampulla, R K Russell
1R. W. Johnson Pharmaceutical Research Institute, Raritan, New Jersey 08869.
Drug Design and Delivery
|October 1, 1990
Abstract:
A synthetic program of rational drug design was undertaken to develop a series of quinazoline-3-oxides as pulmonary-selective inhibitors of ovalbumin-induced, leukotriene-mediated bronchoconstriction. The most active and selective compounds contained a methyl group at the 4-position, a medium sized branched alkyl group at the 2-position, and a small electron donating group on the phenyl ring. Significant enhancement in selectivity was observed in comparing the pulmonary versus cardiovascular effects of these new bronchodilators with the effects of theophylline.