QUANTITATIVE STRUCTURE-ACTIVITY-RELATIONSHIPS IN HISTAMINE H-2-AGONISTS RELATED TO IMPROMIDINE AND ARPROMIDINE

被引：4

作者：

FRANKE, R ^{[1
]}

BUSCHAUER, A ^{[1
]}

机构：

[1] FREE UNIV BERLIN,INST PHARM,W-1000 BERLIN 33,GERMANY

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1992年 / 27卷 / 05期

关键词：

HISTAMINE H-2-RECEPTOR; H-2-AGONISTS; IMPROMIDINE ANALOGS; ARPROMIDINE; QSAR; STRUCTURE-ACTIVITY RELATIONSHIPS;

D O I：

10.1016/0223-5234(92)90178-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Structure-activity relationships for a series of 65 H-2-agonists of the impromidine (phenyl analogues) and arpromidine type were investigated by Free-Wilson analysis. These compounds have in common an imidazolylpropylguanidine moiety which is connected to 1 or 2 aromatic rings through a flexible aliphatic chain which may or may not contain heteroatoms. In one of the rings, substituents are varied in all positions. Free-Wilson analysis revealed that the properties of the side chain and the arrangement of rings are of primary importance for receptor affinity, while substituents showed an irregular pattern of only marginal contributions. The latter is due to the fact that substituent effects are not constant but vary with changes in the chain. This could be verified in a second analysis after introducing appropriate interaction parameters.

引用

页码：443 / 448

页数：6

共 13 条

[1] PHENOXYALKYLGUANIDINE AND PHENYLTHIOALKYLGUANIDINES - SYNTHESIS AND INVITRO PHARMACOLOGY [J].