Synthesis and incorporation of alpha-trifluoromethyl-substituted amino acids into peptides

被引:0
|
作者
Koksch, B [1 ]
Sewald, N [1 ]
Jakubke, HD [1 ]
Burger, K [1 ]
机构
[1] UNIV LEIPZIG,DEPT ORGAN CHEM,D-04103 LEIPZIG,GERMANY
来源
BIOMEDICAL FRONTIERS OF FLUORINE CHEMISTRY | 1996年 / 639卷
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D O I
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中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Methodology for synthesis and incorporation of alpha-trifluoromethyl substituted amino acids into N- and C-terminal position of peptides is described. The incorporation of alpha-trifluoromethyl substituted amino acids into peptides retards proteolytic degradation, enhances lipophilicity, and induces secondary structures. The influence of the trifluoromethyl group on the structure and the receptor affinity of different biologically active peptides (TRH, GnRH, SP) has been studied.
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页码:42 / 58
页数:17
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