Synthesis and pharmacological evaluation of several N-(2-nitrophenyl)piperazine derivatives

Autor: DEANA ANDRIC, GORDANA TOVILOVIC, GORAN ROGLIC, DJURDJICA VASKOVIC, VUKIC SOSKIC, MIRKO TOMIC, SLADJANA KOSTIC-RAJACIC
Jazyk: angličtina
Rok vydání: 2007
Předmět:
Zdroj: Journal of the Serbian Chemical Society, Vol 72, Iss 5, Pp 429-435 (2007)
Druh dokumentu: article
ISSN: 0352-5139
Popis: 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 α1 receptors. All compounds with a benzimidazole group had a 5-HT2A/D2 receptors binding ratio characteristic for atypical neuroleptics (>1, pKi 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.
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