Synthesis and Biological Activity of 5-aryl-4-acyl-3-hydroxy-1-(2-piperazin-1-ylethyl)-2,5-dihydropyrrol-2-ones and their Derivatives

被引：2

作者：

Gein, V. L. ^{[1
]}

Syropyatov, B. Ya. ^{[1
]}

Kasimova, N. N. ^{[1
]}

Dozmorova, N. V. ^{[1
]}

Voronina, E. V. ^{[1
]}

Vakhrin, M. I. ^{[1
]}

机构：

[1] Perm State Pharmaceut Acad, Perm 614600, Russia

来源：

PHARMACEUTICAL CHEMISTRY JOURNAL | 2013年 / 47卷 / 09期

关键词：

5-aryl-4-acyl-3-hydroxy-1-(2-piperazin-1-ylethyl)-2,5-dihydropyrrol-2-ones; 3,4-diaryl-4,6dihydro-5-(2-piperazin-1-ylethyl) pyrrolo[ 3,4-c] pyrazol-6-ones; synthesis; antimicrobial activity; influence on blood coagulation; acute toxicity;

D O I：

10.1007/s11094-013-0986-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

5-Aryl-4-acyl-3-hydroxy-1-(2-piperazin-1-ylethyl)-2,5-dihydropyrrol-2-ones (I) were synthesized by reactions of acylpyruvate methyl esters with a mixture of aromatic aldehyde and 2-(1-piperazino)-1-ethylamine. Then, the corresponding hydrochlorides (II) were obtained. Compounds I were transformed into 3,4-diaryl-4,6-dihydro-5-(2-piperazin-1-ylethyl)pyrrolo[3,4-c]pyrazol-6-ones (III) by reaction with hydrazine hydrate. The antimicrobial activity of compounds I and the influence of compounds II and III on blood coagulation were studied. The acute toxicity of two compounds was evaluated.

引用

页码：485 / 489

页数：5