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N-烷基和N-芳基哌嗪衍生物的合成及其抗菌活性

Synthesis and antimicrobial activity of N-alkyl and N-aryl piperazine derivatives.

作者信息

Chaudhary Preeti, Kumar Rupesh, Verma Akhilesh K, Singh Devender, Yadav Vibha, Chhillar Anil K, Sharma G L, Chandra Ramesh

机构信息

Synthetic Organic Chemistry Research Laboratory, Dr.B. R. Ambedkar Center for Biomedical Research, University of Delhi, Delhi 110007, India.

出版信息

Bioorg Med Chem. 2006 Mar 15;14(6):1819-26. doi: 10.1016/j.bmc.2005.10.032. Epub 2005 Nov 9.

Abstract

A series of substituted piperazine derivatives have been synthesized and tested for antimicrobial activity. The antibacterial activity was tested against Staphylococcus aureus (MTCCB 737), Pseudomonas aeruginosa (MTCCB 741), Streptomyces epidermidis (MTCCB 1824) and Escherichia coli (MTCCB 1652), and antifungal activity against Aspergillus fumigatus, Aspergillus flavus and Aspergillus niger. All synthesized compounds showed significant activity against bacterial strains but were found to be less active against tested fungi. In vitro toxicity tests demonstrated that compounds 4d and 6a showed very less toxicity against human erythrocytes.

摘要

已合成了一系列取代哌嗪衍生物,并对其抗菌活性进行了测试。针对金黄色葡萄球菌(MTCCB 737)、铜绿假单胞菌(MTCCB 741)、表皮葡萄球菌(MTCCB 1824)和大肠杆菌(MTCCB 1652)测试了抗菌活性,针对烟曲霉、黄曲霉和黑曲霉测试了抗真菌活性。所有合成的化合物对细菌菌株均显示出显著活性,但对测试的真菌活性较低。体外毒性测试表明,化合物4d和6a对人红细胞的毒性非常低。

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