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Tropical Journal of Pharmaceutical Research
Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, Nigeria
ISSN: 1596-5996
EISSN: 1596-9827
Vol. 10, No. 3, 2011, pp. 265-272
Bioline Code: pr11035
Full paper language: English
Document type: Research Article
Document available free of charge

Tropical Journal of Pharmaceutical Research, Vol. 10, No. 3, 2011, pp. 265-272

 en Synthesis and Preliminary Pharmacological Evaluation of 2-[4-(Aryl substituted) piperazin-1-yl]-Nphenylacetamides: Potential Antipsychotics
Kumar, Sushil; Wahi, AK & Singh, Ranjit

Abstract

Purpose: Arylpiperazines have been recognized as the largest and most diverse class of compounds exerting actions on the central nervous system with strong affinity for serotonin and dopamine receptors. We here report the synthesis of some novel arylpiperazines and their evaluation for possible antipsychotic properties.
Methods: The target compounds 2-[4-(aryl substituted) piperazin-1-yl]-N-phenylacetamides (3a-j) were synthesized by first reacting aniline (1) in 2 N sodium hydroxide with chloroacetylchloride in dichloromethane to obtain 2-chloro-N-phenylacetamide (2) and subsequently treating with appropriate phenylpiperazine in acetonitrile in the presence of K2CO3 and KI. All the compounds were characterized by analytical and spectroscopic methods. The compounds were evaluated for antipsychotic activity using three animal models.
Results: All the 10 new arylpipeazines showed variable antipsychotic activity with compound 3h being the least effective in the induction of catalepsy. Their effect may involve interaction with 5-HT2A and D2 receptors.
Conclusion: A synthetic method and possible antipsychotic effect have been established for 2-[4-(Aryl substituted) piperazin-1-yl]-N-phenylacetamides.

Keywords
N-phenylacetamide, Arylpiperazines, Antipsychotic activity, 5-HT2A, D2 antagonists

 
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