New. kappa.-receptor agonists based upon a 2-[(alkylamino) methyl] piperidine nucleus

DIC Scopes, NF Hayes, DE Bays, D Belton…

Index: Scopes, David I. C.; Hayes, Norman F.; Bays, David E.; Belton, David; Brain, John; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 3 p. 490 - 501

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Citation Number: 34

Abstract

The syntheaea of some 1-[(3, 4-dichlorophenyl) acetyl]-2-[(a&ylamino) methyl] piperidinea and their activities 88 K-opioid receptor agonists are described. Selected structural modifications are made to the basic moiety and at the 2-, 3-, 4-, 5-, and &positions on the piperidine nucleus to enable structureactivity relationships to be delineated. As a result, some highly potent and selective K-receptor agonists have been identified. In particular, ...