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Report | Regular issue | Vol 22, No. 2, 1984, pp.311-331
Published online, 1st January, 1970
DOI: 10.3987/R-1984-02-0311
■ Benzo- and Indoloquinolizidine Derivatives XIX. The Synthesis and Pharmacologocal Activity of Some Quinolizidine Derivatives, Analogues of Butaclamol

G. Laus, D. Tourwé, and G. Van Binst*

*Laboratoium voor organische Chemie, Vrije Universiteit Brussel, Pleinlaan 2, B-1050 Brussel, Belgium

Abstract

Indenopyridoisoquinoline and benzopyridophenanthridine derivatives were synthesized as the conformationally rigid analogues of butaclamol. For both series, a unique reaction scheme has been worked out in order to obtain the desired trans-cisoid-cis conformation of the end products. In this conformation, the indenopyridoisoquinoline derivative simulates the proposed active form of butaclamol, whilst the benzopyridophenanthridine derivatives simulate the non-active form of butaclamol. The products were tested for neuroleptic activity in “in vitro” models. No significant binding was detected. In view of the pharmacological assays, we cannot decide about the correctness of the proposed structure-activity relationship in the butaclamol series. Overall topological congruence of the phenethylamine part and some flexibility of the system may be important factors for activity.