抗真菌药物的研究Ⅱ．C－端含氧代赖氨酸二肽的合成及抗白念珠菌活性

STUDIES ON ANTIFUNGAL AGENTS Ⅱ.SYNTHESIS AND ANTICANDIDA ALBICANS ACTIVITY OF C-TERMINAL CONTAINING L-4-OXALYSINE DIPEPTIDE

引用违法传递概念设计合成了１１个Ｃ－末端含氧代赖氨酸二肽，进行抗深部致病菌－白念珠菌活性试验，体外实验结果显示极强的抑菌活性，ＭＩＣ在１２．５～０．８μｇ／ｄｉｓｋ之间，较母体氧化赖氨酸大５０～１３５倍（克分子比）。

In order to improve the antifungal effect and the utilitv of L-4-OXalysine(designated as I-677)against clinical pathogen candida albicans,eleven dipeptides with I-677 as C-terminus were designed and synthesized according to the concept of”Illicit Transport“and peptidetransport specifities of C,albicans Anti-C,albicans test in irtro showed that these dipeptides have higheractivitv determined as molar minimum inhibitory concentrations(molar MIC)than that of free I-677by 50～135 fold(as molar MIC)and 31～62 fold(as weight MIC), but less than the N-terminalcontaining I-677 peptides。Mixed anhydride methed was used for the peptide synthesis and the MIC were determined by diskdiffusion assay.