2, 4-Diamino-6, 7-dimethoxyquinazolines. 4. 2-[4-(Substituted oxyethoxy) piperidino] derivatives as. alpha. 1-adrenoceptor antagonists and antihypertensive agents

…, JC Danilewicz, CW Greengrass…

文献索引：Campbell, Simon F.; Danilewicz, John C.; Greengrass, Colin W.; Plews, Rhona M. Journal of Medicinal Chemistry, 1988 , vol. 31, p. 516 - 520

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被引用次数: 8

摘要

A series of 4-amino-6, 7-dimethoxy-2-[4-(substituted oxyethoxy) piperidino] quinazoline derivatives (2) was synthesized and evaluated for a-adrenoceptor affinity and antihypertensive activity. Most compounds showed binding affinities within the nanomolar range for a,-receptors, although 25 and 26 showed enhanced potency (Ki, ca. 1.5 XM), equivalent to that of prazosin. Series 2 also displaced [3H] clonidine from a2- ...