NEW PRENYLAMINE ANALOGS - SYNTHESIS AND CA-2+-ENTRY BLOCKING ACTIVITY

被引:11
作者
CALDIROLA, PM [1 ]
VANDERGOOT, H [1 ]
TIMMERMAN, H [1 ]
机构
[1] FREE UNIV AMSTERDAM,FAC CHEM,DEPT PHARMACOCHEM,BOELELAAN 1083,1081 HV AMSTERDAM,NETHERLANDS
关键词
PRENYLAMINE ANALOGS; CA-ANTAGONISTS; H-3]-NITRENDIPINE DISPLACEMENT; QUALITATIVE SAR;
D O I
10.1016/0223-5234(92)90136-O
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis of a series of diphenylalkylamine derivatives related to prenylamine is reported. The amphetamine group in the prenylamine structure was replaced by other moieties. In addition to substitutions in the aromatic rings, heteroatoms such as sulphur and oxygen were introduced in the chain. The calcium-entry blocking activity was assayed in binding experiments on a guinea-pig brain membrane preparation by displacing [H-3]-nitrendipine.
引用
收藏
页码:571 / 579
页数:9
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