一系列喹唑啉-3氧化物的设计、合成及其支气管扩张活性。

Drug design and delivery Pub Date : 1990-10-01
D W Combs, M S Rampulla, R K Russell, R A Rampulla, D H Klaubert, D Ritchie, A S Meeks, T Kirchner
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引用次数: 0

摘要

我们进行了合理的药物设计合成程序,以开发一系列喹唑啉-3-氧化物作为卵清蛋白诱导的白三烯介导的支气管收缩的肺选择性抑制剂。最具活性和选择性的化合物在4位上含有一个甲基,在2位上含有一个中等大小的支链烷基,在苯基环上含有一个小的给电子基团。在比较这些新的支气管扩张剂与茶碱对肺和心血管的作用时,观察到选择性的显著增强。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Design, synthesis and bronchodilatory activity of a series of quinazoline-3-oxides.

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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