Naphtho and benzo analogues of the kappa opioid agonist trans-(+/-)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl] benzeneacetamide.
Basic Information
ID: ALA1125895
Journal: J Med Chem
Title: Naphtho and benzo analogues of the kappa opioid agonist trans-(+/-)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl] benzeneacetamide.
Authors: Freeman JP, Michalson ET, D'Andrea SV, Baczynskyj L, Von Voigtlander PF, Lahti RA, Smith MW, Lawson CF, Scahill TA, Mizsak SA.
Abstract: Further elaboration on the structure-activity relationships in our U-50,488 series has revealed that benzologation of this cyclohexane-1,2-diamine derivative provides compounds which either maintain the interaction with the kappa receptor (e.g. compounds 3a and 5a in the phenylacetamido series) or eliminate the mu receptor mediated analgesia (e.g. compounds 3-6 in the benzamido series). Naphthologation also caused the elimination of mu receptor mediated analgesia (e.g. compounds 17a and 17b).
CiteXplore: 1648141
DOI: 10.1021/jm00110a021
Patent ID: ┄