取代酚的合成及其抗心律失常和抗副交感神经特性。1. 杂芳胺衍生物。
Synthesis and antiarrhythmic and parasympatholytic properties of substituted phenols. 1. Heteroarylamine derivatives.
作者信息
Stout D M, Matier W L, Barcelon-Yang C, Reynolds R D, Brown B S
出版信息
J Med Chem. 1983 Jun;26(6):808-13. doi: 10.1021/jm00360a005.
PMID:6854583
Abstract
Twenty-four structural derivatives of the antiarrhythmic drug changrolin were synthesized and tested for antiarrhythmic and parasympatholytic activities. It was found that while the bis(pyrrolidinylmethyl)phenol pattern of changrolin appeared to be optimal in this series, a wide latitude existed for the heteroaryl substituent for maintaining good antiarrhythmic activity. Further, the antiarrhythmic and parasympatholytic activities tended to exhibit parallel changes.
摘要
合成了抗心律失常药物常咯啉的24种结构衍生物，并对其抗心律失常和抗副交感神经活性进行了测试。结果发现，虽然常咯啉的双（吡咯烷基甲基）苯酚结构在该系列中似乎是最优的，但对于杂芳基取代基而言，在保持良好抗心律失常活性方面仍有很大的变动范围。此外，抗心律失常和抗副交感神经活性往往呈现平行变化。
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