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N-（2-取代氨基丙酰基）-3-氰基邻氨基苯甲酸甲酯的合成、局部麻醉和抗心律失常活性

Synthesis, local anaesthetic and antiarrhythmic activity of methyl N-(2-substituted aminopropanoyl)-3-cyanoanthranilates.

作者信息

al-Obaid A R

机构信息

Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.

出版信息

Boll Chim Farm. 1996 Jul-Aug;135(7):415-20.

PMID:9035554
Abstract

A series of methyl N-(2-substituted aminopropanoyl)-3-cyanoanthranilates (4a-i), that are structurally-related to tocainide and lidocaine, was synthesized and was found to be active when evaluated for local anaesthetic activity using the frog-foot withdrawal reflex, the guinea pig wheal derm and the rabbit corneal reflex tests. A selected numbers of the series were preliminarily evaluated for antiarrhythmic activity using CaCl2-induced arrhythmia test. Compounds 4a, 4c and 4f at lower doses completely protected the animals against the induced arrhythmias.

摘要

一系列与妥卡尼和利多卡因结构相关的N-（2-取代氨基丙酰基）-3-氰基邻氨基苯甲酸甲酯（4a-i）被合成出来，并且在用青蛙足趾退缩反射、豚鼠风团皮肤和兔角膜反射试验评估局部麻醉活性时被发现具有活性。该系列中的选定数量的化合物使用氯化钙诱导的心律失常试验进行了抗心律失常活性的初步评估。较低剂量的化合物4a、4c和4f完全保护动物免受诱导的心律失常。

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