邻苯二甲酰亚胺与1-甲基乙胺的反应：所得羧酰胺的镇痛和抗炎特性。

Reactions of phthalimides with 1-methylethylamine: analgesic and anti-inflammatory properties of resulting carboxamides.

作者信息

Okunrobo L O, Usifoh C O, Okpo S O

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Benin, Benin City, Nigeria.

出版信息

Pak J Pharm Sci. 2006 Jan;19(1):34-8.

PMID:16632450

Abstract

The reaction of phthalimide derivatives (1a-c) with 1-methylethylamine in dimethylformamide (DMF) at room temperature afforded benzamido-N-prop-2-ynyl-2-(2-methylethyl)-carboxamide (3a), benzamido-N-cyclopentyl-2-(2-methylethyl)-car-boxamide (3b) and benzamido-N-benzyl-2-(2-methylethyl)-carboxamide (3c), respectively. In the carrageenan induced paw oedema test for anti-inflammatory activity, 3a (50 mg/kg) decreased the inflammatory response by 55% after 3 hrs while 3b and 3c exhibited significant reduction in the oedema level. The compounds 3a, 3b and 3c exhibited analgesic activities with 3b producing 76% inhibition. The activities were dose - dependent.

摘要

邻苯二甲酰亚胺衍生物（1a - c）与1 - 甲胺基乙胺在二甲基甲酰胺（DMF）中于室温下反应，分别得到苯甲酰胺基 - N - 丙 - 2 - 炔基 - 2 -（2 - 甲胺基乙） - 羧酰胺（3a）、苯甲酰胺基 - N - 环戊基 - 2 -（2 - 甲胺基乙） - 羧酰胺（3b）和苯甲酰胺基 - N - 苄基 - 2 -（2 - 甲胺基乙） - 羧酰胺（3c）。在角叉菜胶诱导的爪肿胀抗炎活性试验中，3a（50毫克/千克）在3小时后使炎症反应降低了55%，而3b和3c在肿胀水平上有显著降低。化合物3a、3b和3c表现出镇痛活性，其中3b产生了76%的抑制作用。这些活性呈剂量依赖性。