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Updated: Aug 1, 2026

Preparation of Stable Bicyclic Aziridinium Ions and Their Ring-Opening for the Synthesis of Azaheterocycles
Published on: August 22, 2018
Synthesis and dopaminergic features of six novel 3-arylpiperidines
A Kostic-Rajacic1, V Soskic, J Joksimovic
1Institute for Chemistry, Technology and Metallurgy, Njegoseva, Belgrade, Yugoslavia.
Abstract:
Four substituted 3-aryl-1-¿2-[5-(1H-benzimidazole)]ethyl¿piperidines and two 3-aryl-1-¿2-[6-(1,4-dihydroxyquinoxaline-2,3-dione)]ethyl¿ piperidines were synthesized, characterized and evaluated for in vitro binding affinity at the D1 and D2 dopamine and 5-HT1A serotonin receptors using synaptosomal membranes of fresh bovine caudate nuclei and hippocampi as a source of the dopamine and serotonin receptors, respectively, and the corresponding specific radioligands. All six novel compounds expressed no binding affinity at the D1 and 5-HT1A receptors. Derivatives of 1,4-dihydroxyquinoxaline-2,3-dione (compounds 8a and 8b) and of 2-dihalomethylbenzimidazole (ligands 9 and 10) were moderate competitors of [3H]spiperone binding at the D2 dopamine receptors. However, benzimidazole-2-thiones (compounds 7a and 7b) behaved as selective D2 receptor ligands with the binding affinity in the nanomolar range of concentrations.
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