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
收藏
页码：485 / 489
页数：5
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