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色氨酸类似物。1. 位置异构体的合成与降压活性

Tryptophan analogues. 1. Synthesis and antihypertensive activity of positional isomers.

作者信息

Safdy M E, Kurchacova E, Schut R N, Vidrio H, Hong E

出版信息

J Med Chem. 1982 Jun;25(6):723-30. doi: 10.1021/jm00348a022.

DOI:10.1021/jm00348a022
PMID:7097726
Abstract

A series of tryptophan analogues having the carboxyl function at the beta-position was synthesized and tested for antihypertensive activity. The 5-methoxy analogue 46 exhibited antihypertensive activity in the rat via the oral route and was much more potent than the normal tryptophan analogue. The methyl ester was found to be a critical structural feature for activity.

摘要

合成了一系列在β位具有羧基官能团的色氨酸类似物,并对其降压活性进行了测试。5-甲氧基类似物46经口服途径在大鼠中表现出降压活性,且比正常色氨酸类似物的活性强得多。发现甲酯是活性的关键结构特征。

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