Abstract: 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.