2-(3, 4-Dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)-1-substituted-ethyl]-acetamides: the use of conformational analysis in the development of a novel series of …

GF Costello, R James, JS Shaw, AM Slater…

文献索引：Costello, Gerard F.; James, Roger; Shaw, John S.; Slater, Anthony M.; Stutchbury, Neil C. J. Journal of Medicinal Chemistry, 1991 , vol. 34, # 1 p. 181 - 189

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被引用次数: 82

摘要

This paper describes the synthesis of a series of N-[2-(l-pyrrolidinyl) ethyl] acetamides (l), methylated at C1 and/or C2 of the ethyl linking group, and their biological evaluation as opioid K agonists. Conformational analysis of corresponding desaryl analogues 2 suggested that only those compounds capable of occupying an energy minimum close to that of the known K agonist N-[2-(1-pyrrolidinyl) cyclohexyl] acetamide U-50488 might ...