Substituted 1-(aminomethyl)-2-(arylacetyl)-1, 2, 3, 4-tetrahydroisoquinolines: a novel class of very potent antinociceptive agents with varying degrees of selectivity for. …

…, R Colle, G Dondio, G Giardina, G Petrone…

文献索引：Vecchietti; Clarke; Colle; Dondio; Giardina; Petrone; Sbacchi Journal of Medicinal Chemistry, 1992 , vol. 35, # 16 p. 2970 - 2978

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被引用次数: 26

摘要

This study describes the synthesis of a series of novel substituted l-(aminomethyl)-2- (arylacetyl)-l, 2, 3, 4-tetra-hydroisoquinolinea, and discusses their stru-ctiviQ relationships (SARS) using binding affinity for opioid receptors and antinociceptive potency as the indicea of biological adivity. The introduction of a hydroxy substituent in pition 5 of the isoquinoline nucleus generated a compound, 40, which is 2 times more pdent than the previously ...