2-Substituted 1-azabicycloalkanes, a new class of non-opiate antinociceptive agents.
Basic Information
ID: ALA1125504
Journal: J Med Chem
Title: 2-Substituted 1-azabicycloalkanes, a new class of non-opiate antinociceptive agents.
Authors: Carson JR, Carmosin RJ, Vaught JL, Gardocki JF, Costanzo MJ, Raffa RB, Almond HR.
Abstract: 2-Substituted 1-azabicycloalkanes (3- and 5-aryloctahydroindolizines 2 and 11, 3-cyclohexyloctahydroindolizine 12, 4-aryloctahydroquinolizines 13, and 3-arylhexahydropyrrolizines 14) constitute a new class of non-opiate antinociceptive agents. These compounds demonstrated activity in the mouse abdominal constriction test and many were active in the mouse tail-flick test. trans-3-(2-Bromophenyl)octahydroindolizine (2a) did not bind to the opiate receptor nor did it affect arachidonate metabolism. 3-Aryloctahydroindolizines were prepared by catalytic hydrogenation of 1-aryl-3-(2-pyridinyl)-2-propen-1-ones. The X-ray crystal structure of (-)-2a was determined and absolute stereochemistry assigned as 3-R,8a-R.
CiteXplore: 1495016
DOI: 10.1021/jm00093a019
Patent ID: ┄