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Design, synthesis and bronchodilatory activity of a series of quinazoline-3-oxides

Combs, D.W.; Rampulla, M.S.; Russell, R.K.; Rampulla, R.A.; Klaubert, D.H.; Ritchie, D.; Meeks, A.S.; Kirchner, T.

Drug Design and Delivery 6(4): 241-254

1990

ISSN/ISBN: 0884-2884
PMID: 2083028
Document Number: 350851
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.

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