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分子大小对8-羟基-2-(烷基氨基)四氢萘的5-羟色胺受体激动剂活性及美替拉酮类似物对肾上腺皮质11β-羟化酶抑制效力的影响。

Effect of molecular size on 5-hydroxytryptamine receptor agonist activity of 8-hydroxy-2-(alkylamino)tetralins and adrenal cortical 11 beta-hydroxylase inhibition potency of metyrapone analogues.

作者信息

Singh P

出版信息

Arzneimittelforschung. 1986 Oct;36(10):1437-9.

PMID:3493010
Abstract

A quantitative structure-activity relationship has been established between 5-hydroxytryptamine receptor agonist activity of 8-hydroxy-2-(alkylamino)tetralins (I) and adrenal cortical 11 beta-hydroxylase inhibition potency of metyrapone derivatives (II) and the van der Waals volume, Vw, of the compounds. In both examples the size of the molecules has been significantly correlated with the inhibitory potencies of the compounds.

摘要

已在8-羟基-2-(烷基氨基)四氢萘(I)的5-羟色胺受体激动剂活性与美替拉酮衍生物(II)的肾上腺皮质11β-羟化酶抑制效力以及这些化合物的范德华体积Vw之间建立了定量构效关系。在这两个例子中,分子大小与化合物的抑制效力都有显著相关性。

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