AGENTS FOR THE TREATMENT OF OVERACTIVE DETRUSOR .3. SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF N-(4-AMINO-2-BUTYNYL)ACETAMIDE DERIVATIVES

被引：0
|
作者：
TAKE, K
OKUMURA, K
TSUBAKI, K
TERAI, T
SHIOKAWA, Y
机构：
来源：
CHEMICAL & PHARMACEUTICAL BULLETIN | 1992年 / 40卷 / 06期
关键词：
ACETAMIDE; INHIBITORY ACTIVITY; DETRUSOR CONTRACTION; MYDRIASIS; OXYBUTYNIN; OVERACTIVE DETRUSOR; ANTICHOLINERGIC;
D O I：
暂无
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of N-(4-amino-2-butynyl)acetamides were synthesized and examined for their inhibitory activity on detrusor contraction and mydriatic activity as an index of anticholinergic side effect. Among those compounds synthesized, (+)-2-cyclohexyl-N-(4-dimethylamino-2-butynyl)-2-hydroxy-2-phenylacetamide hydrochloride ((+)-13b . HCl), 2-cyclohexyl-2-hydroxy-N-(4-methylamino-2-butynyl)-2-phenylacetamide hydrochloride (13c . HCl), N-(4-dimethylamino-2-butynyl)-2,2-diphenyl-2-hydroxyacetamide hydrochloride (14a . HCl), and 2,2-diphenyl-N-(4-ethylamino-2-butynyl)-2-hydroxyacetamide hydrochloride (14b . HCl) showed equipotent inhibitory activity on detrusor contraction to oxybutynin (1) and less mydriatic activity. Further evaluation of these compounds as an agent for the treatment of overactive detrusor has been examined.
引用
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页码：1415 / 1423
页数：9
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