Preparation and opioid activity of analogs of the analgesic dipeptide 2, 6-dimethyl-L-tyrosyl-N-(3-phenylpropyl)-D-alaninamide

…, E Rorbacher, PC Contreras, D Hammond

Index: Chandrakumar; Yonan; Stapelfeld; Savage; Rorbacher; Contreras; Hammond Journal of Medicinal Chemistry, 1992 , vol. 35, # 2 p. 223 - 233

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Citation Number: 42

Abstract

A number of analogues of the recently disclosed analgesic dipeptide 2, 6-dimethyl-~-tyrcsyl- ~-alanine-phenylpropylamide (SC-39566, 2) were prepared. These analogues contained oxymethylene, aminomethylene, ketomethylene, bismethylene, and trans double bond (including vinyl fluoride) isosteric replacements for the amide bond between the D-alanine and phenylpropylamine units in 2. These compounds were tested in opioid binding ...