SYNTHESIS OF 2-[[1-OXO-2-(SUBSTITUTED AMINO)PROPYL]AMINO]-4,5,6,7-TETRAHYDROBENZO[B]THIOPHEN-3-CARBOXYLIC ACID ETHYL-ESTERS AS POTENTIAL LOCAL-ANESTHETIC AGENTS

被引：0
|
作者：
ALOBAID, ARMA
机构：
来源：
ARZNEIMITTEL-FORSCHUNG/DRUG RESEARCH | 1995年 / 45-1卷 / 05期
关键词：
ANESTHETICS; LOCAL; CARTICAINE; LIDOCAINE; 2-[[1-OXO-2-(SUBSTITUTED AMINO)PROPYL]AMINO]-4,5,6,7-TETRAHYDROBENZO[B]THIOPHEN-3-CARBOXYLIC ACID, ETHYL ESTERS, PHARMACOLOGY, SYNTHESIS;
D O I：
暂无
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The synthesis of a series of 10 compounds related to 2-[[1-oxo-2-substituted amino)propyl]amino]-4,5,6,7-tetrahydrobenzo[b]thiophen-3-carboxylic acid ethyl esters (III-XII) that are structurally-related to carticaine and the results of a study of their biological activity are reported Most of the these compounds showed significant activity at lower concentrations when evaluated for local anesthetic activity using the frog-foot withdrawal reflex, the guinea pig wheal derm and the rabbit corneal reflex tests. Compounds III, V, VII and X displayed the shortest onset times and the longest duration of activity, compared to the model drug lidocaine.
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页码：627 / 630
页数：4
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