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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
引用本文:黄嘉鑫,陈岚,奚明磊,林巍,方佩芬,张鸿龙,顾秀玉. 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[J]. 药学学报, 1996, 31(1): 24-28
作者姓名:黄嘉鑫  陈岚  奚明磊  林巍  方佩芬  张鸿龙  顾秀玉
作者单位:中国科学院上海药物研究所,上海 200031
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。

关 键 词:氧代赖氨酸  违法传递  抗真菌
收稿时间:1995-03-01

ON ANTIFUNGAL AGENTS Ⅱ.SYNTHESIS AND ANTICANDIDA ALBICANS ACTIVITY OF C-TERMINAL CONTAINING L-4-OXALYSINE DIPEPTIDE
JX Huang,L Chen,ML Xi,W Lin,PF Fang,HL Zhang and XY Gu. ON ANTIFUNGAL AGENTS Ⅱ.SYNTHESIS AND ANTICANDIDA ALBICANS ACTIVITY OF C-TERMINAL CONTAINING L-4-OXALYSINE DIPEPTIDE[J]. Acta pharmaceutica Sinica, 1996, 31(1): 24-28
Authors:JX Huang  L Chen  ML Xi  W Lin  PF Fang  HL Zhang  XY Gu
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.
Keywords:Illicit transport  Antifungal  L-4-oxalysine(I-677)
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