SYNTHESIS OF 2,3,4,4A,5,9B-HEXAHYDRO-1H-PYRIDO[4,3-B]INDOLE DERIVATIVES AND THEIR CENTRAL NERVOUS-SYSTEM ACTIVITIES

The synthesis and some pharmacological effects of cis-and (rans-2-substituted 2, 3, 4, 4a, 5, 9b-hexahydro-l/f-pyrido[4, 3-b]indole derivatives are described. In these derivatives, the substituents of the 2, 5 and 8 position, together with the relative configuration of the 4a and 9b position, influenced the potency of the central nervous system activities.A ci5-2-[3-(p-fluorobenzoyl)propyl] analogue (5k) of carbidine (1) possessed not only thymoleptic-like biological activity but had more potent neuroleptic activity than the parent drug. © 1979, American Chemical Society. All rights reserved.