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新型1,3,5-三嗪衍生物作为抗菌剂的合成与生物学评价

Synthesis and biological evaluation of novel 1,3,5-triazine derivatives as antimicrobial agents.

作者信息

Zhou Chunhui, Min Jaeki, Liu Zhigang, Young Anne, Deshazer Heather, Gao Tian, Chang Young-Tae, Kallenbach Neville R

机构信息

Department of Chemistry, New York University, 100 Washington Square East, New York, NY 10003, USA.

出版信息

Bioorg Med Chem Lett. 2008 Feb 15;18(4):1308-11. doi: 10.1016/j.bmcl.2008.01.031. Epub 2008 Jan 11.

DOI:10.1016/j.bmcl.2008.01.031
PMID:18226902
Abstract

Numerous studies have contributed to the development of natural and synthetic antimicrobial peptides as a prospective source of antibiotic agents. Based on the concept that cationic charge, bulk, and lipophilicity are major factors determining antibacterial activity in these peptides, we designed and screened several combinatorial libraries based on 1,3,5-triazine as a template. A set of compounds were identified to show potent antimicrobial activity together with low hemolytic activity.

摘要

众多研究推动了天然和合成抗菌肽的发展,使其成为抗生素药物的潜在来源。基于阳离子电荷、体积和亲脂性是决定这些肽抗菌活性的主要因素这一概念,我们以1,3,5-三嗪为模板设计并筛选了几个组合文库。鉴定出一组化合物,它们具有强效抗菌活性且溶血活性低。

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