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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

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【作者】 黄嘉鑫陈岚奚明磊林巍方佩芬张鸿龙顾秀玉

【Author】 JX Huang;L Chen;ML Xi;W Lin;PF Fang;HL Zhang and XY Gu(Shanghai Institute of Materia Medica,Academia Sinica,shanghai 200031)

【机构】 中国科学院上海药物研究所

【摘要】 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)。

【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.

【关键词】 氧代赖氨酸违法传递抗真菌
【Key words】 L-4-oxalysine(I-677)Illicit transportAntifungal
  • 【文献出处】 药学学报 ,ACTA PHARMACEUTICA SINICA , 编辑部邮箱 ,1996年01期
  • 【分类号】R914.5
  • 【下载频次】75
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