SYMBIOTIC APPROACH TO DRUG DESIGN - N-[(4-CHLORO-3-SULFAMOYLBENZAMIDO)-ETHYL]PROPANOLAMINE DERIVATIVES AS BETA-ADRENERGIC BLOCKING-AGENTS WITH DIURETIC ACTIVITY

被引:7
作者
CECCHETTI, V
SCHIAFFELLA, F
TABARRINI, O
ZHOU, W
FRAVOLINI, A
GOI, A
BRUNI, G
SEGRE, G
机构
[1] UNIV PERUGIA,IST CHIM FARMACEUT & TECN FARMACEUT,I-06100 PERUGIA,ITALY
[2] SOC PROD ANTIBIOT SPA,I-20143 MILAN,ITALY
[3] UNIV SIENA,IST FARMACOL,I-53100 SIENA,ITALY
关键词
OXYPROPANOLAMINES; IMINOXYPROPANOLAMINES; BETA-BLOCKING-DIURETIC ACTIVITY; ANTIHYPERTENSIVE ACTIVITY;
D O I
10.1016/0223-5234(91)90098-8
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of oxypropanolamines and iminoxypropanolamines, in which the aminic substituent was the 2-(4-chloro-3-sulfamoylbenzamido)-ethyl group, were synthesized as potential beta-blocker/diuretic agents. All of these compounds were tested for beta-1-adrenoceptor affinity and beta-blocking potency. For the most active compounds, diuretic and antihypertensive properties as well as affinity for alpha-1-adrenoceptors were also investigated. Compounds 4 and 10 were found to display contemporaneously beta-blocking, diuretic and antihypertensive activities.
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页码:381 / 386
页数:6
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