Abstract
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
Letters in Drug Design & Discovery
Title: Synthesis and Computational Studies on Aryloxypropyl Piperazine Derivatives as Potential Atypical Antipsychotic Agents
Volume: 9 Issue: 2
Author(s): Alka Bali, Abhishek Bhalla, Suman Bala and Rajesh Kumar
Affiliation:
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
Abstract: 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.
Export Options
About this article
Cite this article as:
Bali Alka, Bhalla Abhishek, Bala Suman and Kumar Rajesh, Synthesis and Computational Studies on Aryloxypropyl Piperazine Derivatives as Potential Atypical Antipsychotic Agents, Letters in Drug Design & Discovery 2012; 9 (2) . https://dx.doi.org/10.2174/157018012799079725
DOI https://dx.doi.org/10.2174/157018012799079725 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
MicroRNA miR-122 as a Therapeutic Target for Oligonucleotides and Small Molecules
Current Medicinal Chemistry Novel Classes of Dimer Antitumour Drug Candidates
Current Pharmaceutical Design Roles of Secreted Phospholipases A<sub>2</sub> in the Mammalian Immune System
Protein & Peptide Letters Graphical Abstracts
Letters in Drug Design & Discovery Hydrogen Gas Therapy: From Preclinical Studies to Clinical Trials
Current Pharmaceutical Design Pharmacotherapy of Acute Lung Injury and Acute Respiratory Distress Syndrome
Current Medicinal Chemistry Application of Molecular Imaging Technologies in Antitumor Drug Development and Therapy
Current Pharmaceutical Design Advances in Peptide-based DNA/RNA-Intercalators
Current Protein & Peptide Science Editorial [Hot Topic: NMDA Receptors as Targets in Medicinal Chemistry (Guest Editor: Dr. William Metz)]
Current Topics in Medicinal Chemistry Neurological Effects of SARS-CoV-2 and Neurotoxicity of Antiviral Drugs Against COVID-19
Mini-Reviews in Medicinal Chemistry New Anti-Tuberculosis Drugs with Novel Mechanisms of Action
Current Medicinal Chemistry Antioxidant Effect of Flavonoids Present in Euterpe oleracea Martius and Neurodegenerative Diseases: A Literature Review
Central Nervous System Agents in Medicinal Chemistry Unsaturation: An Important Structural Feature to Nucleosides’ Antiviral Activity
Anti-Infective Agents SARS-CoV-2: Impacts and Echoes
Reviews on Recent Clinical Trials How Large Does a Compound Screening Collection Need To Be?
Combinatorial Chemistry & High Throughput Screening Mechanism of Conjugated Imine and Iminium Species, including Marine Alkaloids: Electron Transfer, Reactive Oxygen Species, Therapeutics and Toxicity
Current Bioactive Compounds Hydroxychloroquine Induced DRESS (Drug Rash with Eosinophilia and Systemic Symptoms Syndrome) Mimicking SARS-COV-2 Illness: A Case Report with Review
Coronaviruses Assessment of the Antineoplastic Potential of Chalcones in Animal Models
Current Medicinal Chemistry Structure-Activity Relationships of Flavonoids
Current Organic Chemistry The β-Carbonic Anhydrases from Mycobacterium tuberculosis as Drug Targets
Current Pharmaceutical Design