抗真菌药物的研究VI.C-端含MEDP的寡肽的合成和抗白念珠菌活性

STUDIES ON ANTIFUNGAL AGENTS VI. SYNTHESIS AND ANTICANDIDAALBICANS ACTIVITY OF CTERMINAL CONTAINING MEDP PEPTIDES

摘要: 目的:寻找高效低毒的抗真菌化合物。方法和结果:根据违法传递概念设计合成了12个碳端含有MEDP(N³-(2R,3R)-4-methoxyepoxysucinyl-L-2,3-diaminopropanoicacid)的二肽和三肽(1～12),均系新化合物。结论:体外抗白念珠菌实验表明:有些二肽三肽体外实验显示了较强的抑菌活性,其中ValMEDP的活性最强,其MMIC为45nmol·mL^-1,较母体MEDP提高960倍。

Abstract: AIM: To search for compounds having strong antifungal activities. METHODS AND RESULTS: Twelve new peptides containing MEDP(N³-(2-R,3R)-4-methoxyepoxysuccinyl-L-2,3-diaminopropanoic acid) in Cterminus have been synthesized and evaluated in vitro against Candida albicans on the basis of “illicit transport”. CONCLUSION: Some of them have strong activities. The MMIC(molar mininum inhibitory concentrations) of ValMEDP, the most active peptide in this series, is 448 nmol·mL^-1, 960 times the MMIC of MEDP. But all of the peptides showed weaker activities than the related peptides containing FMDP(N³-4-methoxyfumaryl-L-2,3-diaminopropanoic acid).