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2, 4-Diamino-6, 7-dimethoxyquinazolines. 1. 2-[4-(1, 4-Benzodioxan-2-ylcarbonyl) piperazin-1-yl] derivatives as. alpha. 1-adrenoceptor antagonists and …

SF Campbell, MJ Davey, JD Hardstone…

文献索引:Campbell; Davey; Hardstone; Lewis; Palmer Journal of Medicinal Chemistry, 1987 , vol. 30, # 1 p. 49 - 57

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被引用次数: 102

摘要

A series of 4-amino-2-[4-(1, 4-benzodioxan-2-ylcarbonyl) piperazin-l-yl]-6, 7- dimethoxyquinazoline derivatives was synthesized for evaluation as a-antagonists and antihypertensive agents. Most compounds displayed high (nM) binding affinity for a,- adrenoceptors with no significant activity at a2-sites. Selective antagonism of the a,- mediated vasoconstrictor effects of norepinephrine is also characteristic of the series. ...