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Journal of the Serbian Chemical Society 2007 Volume 72, Issue 5, Pages: 429-435
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Synthesis and pharmacological evaluation of several N-(2-nitrophenyl) piperazine derivatives

Andrić Deana, Tovilović Gordana, Roglić Goran, Vasković Đurđica, Šoškić Vukić, Tomić Mirko, Kostić-Rajačić Slađana

Six newly synthesized heterocyclic (2-nitrophenyl)piperazines, with a specific structure of the heteroaryl group, whichmimics the catechol moiety of dopamine (benzimidazoles and substituted benzimidazoles), were evaluated for their binding affinity to rat dopamine (DA), serotonin (5-HT) and _1 receptors. All compounds with a benzimidazole group had a 5-HT2A/D2 receptors binding ratio characteristic for atypical neuroleptics (>1, pK i values). Compound 7c, 4-bromo-6-{2-_4-(2-nitrophenyl)piperazin- 1-yl_ethyl}-1H-benzimidazole, expressed higher affinities for all receptor classes than clozapine. Also, it exhibited the best characteristic for atypical neuroleptics and presents a compound with the best profile for further in vivo investigations.

Keywords: arylpiperazines, benzimidazoles, dopamine receptors, serotonin receptors, atypical antipsychotic