Gupta R C, Mukerji S, Chatterjee S K, Rastogi S N, Anand N, Dube M P, Sur R N, Mukerji K C, Srimal R C
Arzneimittelforschung. 1978;28(2):241-6.
The synthesis and pharmacological activity of some 3-tertiary amino-1-aryloxy- or 1-aryl-, 1-thiophenoxy and 1-anilino-propan-2-ols and -propanes, particularly those derived from N-phenylpiperazines are described. Effect of substituents (nature/position) on the phenyl ring, the phenoxy ring as well as alteration in the hydroxylic function vis-à-vis the structure-activity relationships (SAR) are discussed. In general, the 1-aryloxy compounds have hypotensive activity--this being more pronounced in those carrying an o-substituent on the phenyl ring, while m and p-substituted derivatives have their effect primarily on the CNS. Variations in the phenoxy moiety do not significantly alter the intrinsic activity. The 1-aryl compounds, on the other hand, have significant CNS activity, which is markedly affected by the substituents on the 1-aryl residue.
本文描述了一些3-叔氨基-1-芳氧基或1-芳基、1-噻吩氧基和1-苯胺基丙-2-醇及丙烷的合成与药理活性，特别是那些源自N-苯基哌嗪的化合物。讨论了苯环、苯氧基上取代基的性质/位置以及羟基功能的改变对构效关系（SAR）的影响。一般来说，1-芳氧基化合物具有降压活性——在苯环上带有邻位取代基的化合物中这种活性更为明显，而间位和对位取代的衍生物主要作用于中枢神经系统。苯氧基部分的变化不会显著改变内在活性。另一方面，1-芳基化合物具有显著的中枢神经系统活性，这受到1-芳基残基上取代基的显著影响。
