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.
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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