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

作　　者：高旭日[1] 黄嘉鑫 蔡俊超[1] 

机构地区：[1]中国科学院上海药物研究所

出　　处：《药学学报》1999年第7期505-509,共5页Acta Pharmaceutica Sinica

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。AIM: To search for compounds having strong anti fungal activities. METHODS AND RESULTS: Twelve new peptides containing MEDP(N 3 [(2 R ,3 R ) 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(N 3 4 methoxyfumaryl L 2,3 diaminopropanoic acid).

关 键 词：MEDP 氧代赖氨酸 抗真菌药 

分 类 号：R978.5[医药卫生—药品]