Synthesis of pseudopeptides based l-tryptophan as a potential antimicrobial agent
- 作者：Jian Lv ; Liang Yin ; Tingting Liu ; Yongmei Wang
- 关键词：Pseudopeptides ; l-Tryptophan ; Antimicrobial activity ; Haemolytic assay
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2007
- 期刊代码：10_0960894x
- 类别：ch
- 出版时间：15 March 2007
- 卷：17
- 期：6
- 页码：1601-1607
- 文件大小：172 K
摘要
Four compounds named l-BTrpPA, l-Trp-o-PA, l-Trp-m-PA and l-Trp-p-PA, pseudopeptides constructed from pyridine and tryptophan units, were synthesized and tested against the Gram-positive, Gram-negative strains of bacteria and human pathogenic fungi. l-Trp-o-PA proved to be a broad-spectrum antimicrobial agent, showing a significant inhibition of the growth of Gram-positive bacteria (Staphylococcus aureus, methicillin-resistant S. aureus, Bacillus subtilis, Micrococcus luteus), and pathogenic fungi (Candida spp., Cryptococcus neoformans, Rhodotorula glutinis, Saccharomyces cerevisiae, Aspergillus spp., Rhizopus nigricans) tested and activity against Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa and Proteus vulgaris, Enterobacter aerogenes) tested. The in vitro cell cytotoxicity of l-Trp-o-PA was evaluated using haemolytic assay, in which the compound was found to have low lytic property, even up to the concentration of 4000 μg/mL, it only lysed 6–7%of erythrocytes, which was 100-fold greater than the MICs (minimum inhibitory concentration).