Deparment of Chemistry, University of Salerno, Via Ponte Don Melillo, 84084 Fisciano (SA), Italy.
Bioorg Med Chem. 2010 Mar 1;18(5):2010-8. doi: 10.1016/j.bmc.2010.01.026. Epub 2010 Jan 15.
The synthesis and screening of neutral and cationic, linear and cyclic peptoids (N-alkylglycine peptidomimetics) is described. Structure-activity relationship studies show that the in vitro activities of the tested peptoids depend on both cyclization and decoration with cationic groups. The most powerful N-lysine cyclopeptoid derivatives showed good antifungal activity against Candida albicans (ATCC90029 and L21) and Candida famata (SA550, Amph B-resistant) and low hemolytic activity. The effects of the cyclic peptoids on membrane permeabilization were evaluated by the propidium iodide exclusion assay.
描述了中性和阳离子型、线性和环状肽（N-烷基甘氨酸肽模拟物）的合成和筛选。构效关系研究表明，所测试的肽的体外活性取决于环化和阳离子基团的装饰。最有效的 N-赖氨酸环肽衍生物对白色念珠菌（ATCC90029 和 L21）和假丝酵母（SA550，两性霉素 B 耐药）表现出良好的抗真菌活性，且溶血活性低。通过碘化丙啶排除试验评估了环状肽对膜通透性的影响。
