氮丙啶衍生物的研究。II. α-氮丙啶基-β-/对氯苯甲酰基/-丙酸取代酰胺和取代苯胺的合成及免疫药理学分析。

Studies on the derivatives of aziridine. II. Synthesis and immunopharmacological analysis of substituted amides and anilides of alpha-aziridinyl-beta-/p-chlorobenzoyl/-propionic acid.

作者信息

Zabska R, Kowalczyk-Bronisz S H

机构信息

Department of Chemistry of Drug, Medical Academy, Wrocøaw.

出版信息

Arch Immunol Ther Exp (Warsz). 1987;35(5):681-91.

Abstract

Several new amides and anilides of alpha-aziridinyl-beta-/p-chlorobenzoyl/-propionic acid were synthetized. The beta-/p-chlorobenzoyl/-acrylic acid 2 was used as the substrate. This compound was converted by reaction with appropriate amine into amides and anilides of beta-/p-chlorobenzoyl/-acrylic acid (3-10). These compounds react with ethylenoimine giving appropriate amides and anilides of alpha-aziridinyl-beta-/p-chlorobenzoyl/-propionic acid (11-18). When pharmacologically analyzed, they appeared to possess marked immunotropic activity. The derivatives in question modulated both humoral as well as cellular immune response, the effect being related to the type of substitutent in the amide group.

摘要

合成了几种新型的α-氮丙啶基-β-/对氯苯甲酰基/-丙酸的酰胺和酰苯胺。以β-/对氯苯甲酰基/-丙烯酸2作为底物。该化合物通过与适当的胺反应转化为β-/对氯苯甲酰基/-丙烯酸的酰胺和酰苯胺（3 - 10）。这些化合物与乙烯亚胺反应，得到相应的α-氮丙啶基-β-/对氯苯甲酰基/-丙酸的酰胺和酰苯胺（11 - 18）。经药理分析，它们似乎具有显著的免疫调节活性。所讨论的衍生物调节体液免疫和细胞免疫反应，其效果与酰胺基团中取代基的类型有关。

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