Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


Synthesis and Computational Studies on Aryloxypropyl Piperazine Derivatives as Potential Atypical Antipsychotic Agents

Author(s): Alka Bali, Abhishek Bhalla, Suman Bala, Rajesh Kumar.


A series of aryloxypropyl derivatives have been synthesized and evaluated for atypical antipsychotic activity in apomorphine induced mesh climbing and stereotypy assays in mice and the compounds displayed good efficacy coupled with an atypical profile. Investigation of the selected physicochemical parameters important for CNS activity suggested a good potential for CNS activity. All compounds showed excellent compliance with lipinskis rules for oral and CNS activity. Good physicochemical similarity was noted for the test compounds with respect to standard drugs and good brain permeation was suggested by their log BB values computed through an online software program.

Keywords: Atypical antipsychotics, CNS agents, Lipinski rules, Log BB, Aryloxypiperazines, Piperazine, aryloxypropyl derivatives, CNS activity, physicochemical similarity, Schizophrenia, Neurochemical, dopaminergic hypothesis, mesocorticolimbic system, bradykinesia, akathesia, nigrostriatal pathway

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Article Details

Year: 2012
Page: [218 - 224]
Pages: 7
DOI: 10.2174/157018012799079725
Price: $58