Selective. kappa.-Opioid Agonists: Synthesis and Structure-Activity Relationships of Piperidines Incorporating an Oxo-Containing Acyl Group

…, G Petrone, M Sbacchi, V Vecchietti

Index: Giardina; Clarke; Dondio; Petrone; Sbacchi; Vecchietti Journal of Medicinal Chemistry, 1994 , vol. 37, # 21 p. 3482 - 3491

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Citation Number: 29

Abstract

This study describes the synthesis and the structure-activity relationships (SARs) of the (S)-(- )-enantiomers of a novel class of 24 aminomethy1) piperidine derivatives, using K-opioid binding anity and antinociceptive potency as the indices of biological activity. Compounds incorporating the 1-tetralon-6-ylacetyl residue (30 and 34-45) demonstrated an in vivo antinociceptive activity greater than predicted on the basis of their K-binding affinities. In ...