Structure activity studies related to 2-(3, 4-dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)-1-substituted-ethyl] acetamides: a novel series of potent and selective. kappa. …

…, TP Blackburn, GF Costello, R James…

Index: Barlow, Jeffrey J.; Blackburn, Thomas P.; Costello, Gerard F.; James, Roger; Count, David J. Le; et al. Journal of Medicinal Chemistry, 1991 , vol. 34, # 11 p. 3149 - 3158

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Citation Number: 43

Abstract

This paper describes the synthesis of a series of N-[2-(1-pyrrolidinyl) ethyl] acetamides 1, variously substituted at the carbon adjacent to the amide nitrogen (Cl), and related analogues, together with their biological evaluation as opioid K agonists. In the first part of the study, the variants in N-acyl, N-alkyl, and amino functions were explored when the substituent at C1 was 1-methylethyl and the optimum was found to be exemplified by 2-(3, ...