1, 3-Diamino-6, 7-dimethoxyisoquinoline derivatives as potential. alpha. 1-adrenoceptor antagonists

J Bordner, SF Campbell, MJ Palmer…

文献索引：Bordner, Jon; Campbell, Simon F.; Palmer, Michael J.; Tute, Michael S. Journal of Medicinal Chemistry, 1988 , vol. 31, # 5 p. 1036 - 1039

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被引用次数: 23

摘要

Treatment of 2-methyl-4, 5-dimethoxybenzonitrile (3) with LDA followed by reaction with an N, N-disubstituted cyanamide provided a series of 1, 3-diamino-6, 7-dimethoxyisoquinolines (2), which were evaluated for a-adrenoceptor binding affinity and antihypertensive activity. l- Amino-3-(dimethylamino)-6, 7-dimethoxyisoquinoline(4) showed no significant affinity (Ki>> lo4 M) for e,-adrenoceptors, while the corresponding 3-(2-furoylpiperazin-l-yl) analogue (8 ...