Synthesis, Computational Studies and Preliminary Pharmacological Evaluation of New Arylpiperazines

A series of novel arylpiperazines were synthesized and the target compounds evaluated for atypical antipsychotic activity in apomorphine induced climbing behavior (D2 antagonism), 5-HTP induced head twitches (5-HT2A antagonism) and catalepsy studies in albino mice. The physicochemical similarity of...

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Main Authors: Sushil Kumar, A. K. Wahi, Ranjit Singh
Format: Article
Language:English
Published: Wiley 2011-01-01
Series:E-Journal of Chemistry
Online Access:http://dx.doi.org/10.1155/2011/346087
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author Sushil Kumar
A. K. Wahi
Ranjit Singh
author_facet Sushil Kumar
A. K. Wahi
Ranjit Singh
author_sort Sushil Kumar
collection DOAJ
description A series of novel arylpiperazines were synthesized and the target compounds evaluated for atypical antipsychotic activity in apomorphine induced climbing behavior (D2 antagonism), 5-HTP induced head twitches (5-HT2A antagonism) and catalepsy studies in albino mice. The physicochemical similarity of the target compounds with respect to standard drugs clozapine, ketanserine and risperidone was assessed by calculating from a set of physiochemical properties using software programs. The test compounds (3a-j) demonstrated good similarity values with respect to the standard drugs. Among them, compound 3d has emerged as an important lead compound showing potential atypical antipsychotic like profile.
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spelling doaj-art-0e2f83c190d44dd796f68b74326d4c502025-02-03T06:08:14ZengWileyE-Journal of Chemistry0973-49452090-98102011-01-01831044105110.1155/2011/346087Synthesis, Computational Studies and Preliminary Pharmacological Evaluation of New ArylpiperazinesSushil Kumar0A. K. Wahi1Ranjit Singh2Drug Design & Medicinal Chemistry Research Laboratory, College of Pharmacy, IFTM, Moradabad-244001, IndiaDrug Design & Medicinal Chemistry Research Laboratory, College of Pharmacy, IFTM, Moradabad-244001, IndiaSchool of Pharmaceutical Sciences, Shobhit University, Meerut, IndiaA series of novel arylpiperazines were synthesized and the target compounds evaluated for atypical antipsychotic activity in apomorphine induced climbing behavior (D2 antagonism), 5-HTP induced head twitches (5-HT2A antagonism) and catalepsy studies in albino mice. The physicochemical similarity of the target compounds with respect to standard drugs clozapine, ketanserine and risperidone was assessed by calculating from a set of physiochemical properties using software programs. The test compounds (3a-j) demonstrated good similarity values with respect to the standard drugs. Among them, compound 3d has emerged as an important lead compound showing potential atypical antipsychotic like profile.http://dx.doi.org/10.1155/2011/346087
spellingShingle Sushil Kumar
A. K. Wahi
Ranjit Singh
Synthesis, Computational Studies and Preliminary Pharmacological Evaluation of New Arylpiperazines
E-Journal of Chemistry
title Synthesis, Computational Studies and Preliminary Pharmacological Evaluation of New Arylpiperazines
title_full Synthesis, Computational Studies and Preliminary Pharmacological Evaluation of New Arylpiperazines
title_fullStr Synthesis, Computational Studies and Preliminary Pharmacological Evaluation of New Arylpiperazines
title_full_unstemmed Synthesis, Computational Studies and Preliminary Pharmacological Evaluation of New Arylpiperazines
title_short Synthesis, Computational Studies and Preliminary Pharmacological Evaluation of New Arylpiperazines
title_sort synthesis computational studies and preliminary pharmacological evaluation of new arylpiperazines
url http://dx.doi.org/10.1155/2011/346087
work_keys_str_mv AT sushilkumar synthesiscomputationalstudiesandpreliminarypharmacologicalevaluationofnewarylpiperazines
AT akwahi synthesiscomputationalstudiesandpreliminarypharmacologicalevaluationofnewarylpiperazines
AT ranjitsingh synthesiscomputationalstudiesandpreliminarypharmacologicalevaluationofnewarylpiperazines