alexa Molecular Docking, Synthesis and Biological Evaluation of Some Novel 2-Substituted-3-allyl-4(3H)-quinazolinone Derivatives as Anticonvulsant Agents | OMICS International | Abstract
ISSN: 2161-0444

Medicinal Chemistry
Open Access

Like us on:
OMICS International organises 3000+ Global Conferenceseries Events every year across USA, Europe & Asia with support from 1000 more scientific Societies and Publishes 700+ Open Access Journals which contains over 50000 eminent personalities, reputed scientists as editorial board members.

Open Access Journals gaining more Readers and Citations

700 Journals and 15,000,000 Readers Each Journal is getting 25,000+ Readers

This Readership is 10 times more when compared to other Subscription Journals (Source: Google Analytics)

Research Article

Molecular Docking, Synthesis and Biological Evaluation of Some Novel 2-Substituted-3-allyl-4(3H)-quinazolinone Derivatives as Anticonvulsant Agents

Hamada S Abulkhair1, Kamal M El-Gamal1,2, Khaled El-Adl3* and Mohamed F Fadl4

1Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Nasr City 11884, Cairo, Egypt

2Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy and Pharmaceutical Industries, Delta University, Mansoura, Egypt

3Pharmaceutical Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Nasr City 11884, Cairo, Egypt

4Pharmacology and Toxicology Department, Faculty of Pharmacy, Al-Azhar University, Nasr City 11884, Cairo, Egypt

*Corresponding Author:
Khaled El-Adl
Assistant Professor of Pharmaceutical Chemistry
Faculty of Pharmacy, Al-Azhar University
Cairo, Egypt
Tel: +20224018031
E-mail: [email protected]

Received date: September 23, 2016; Accepted date: September 29, 2016; Published date: September 30, 2016

Citation: Abulkhair HS, El-Gamal KM, El-Adl K, Fadl MF (2016) Molecular Docking, Synthesis and Biological Evaluation of Some Novel 2-Substituted-3-allyl-4(3H)- quinazolinone Derivatives as Anticonvulsant Agents. Med Chem (Los Angeles) 6:593-603. doi:10.4172/2161-0444.1000404

Copyright: © 2016 Abulkhair HS, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

Abstract

A new series of 2-substituted-3-allyl-4(3H)-quinazolinone derivatives (4a-e-8a-d) were synthesized and evaluated for their anticonvulsant activity against pentylenetetrazole (PTZ)-induced seizures and maximal electroshock test in mice and compared with the reference drugs methaqualone and sodium valproate. The neurotoxicity was assessed using rotarod test. The molecular modeling was performed for all synthesized compounds to predict their binding affinity towards GABA-A receptor as a proposed mode of their anticonvulsant activity. The data obtained from the molecular docking was strongly correlated with that obtained from the biological screening which revealed that; compounds 4c, 4b and 4d showed the highest binding affinities towards GABA-A receptor and also showed the highest anticonvulsant activities in experimental mice with relatively low neurotoxicity and low toxicity in the median lethal dose test when compared with the reference drugs. The obtained results proved that the most active compounds could be useful as a model for future design, adaptation and investigation to construct more active analogs.

Keywords

Peer Reviewed Journals
 
Make the best use of Scientific Research and information from our 700 + peer reviewed, Open Access Journals
International Conferences 2018-19
 
Meet Inspiring Speakers and Experts at our 3000+ Global Annual Meetings

Contact Us

Agri & Aquaculture Journals

Dr. Krish

[email protected]

1-702-714-7001Extn: 9040

Biochemistry Journals

Datta A

[email protected]

1-702-714-7001Extn: 9037

Business & Management Journals

Ronald

[email protected]

1-702-714-7001Extn: 9042

Chemistry Journals

Gabriel Shaw

[email protected]micsonline.com

1-702-714-7001Extn: 9040

Clinical Journals

Datta A

[email protected]

1-702-714-7001Extn: 9037

Engineering Journals

James Franklin

[email protected]

1-702-714-7001Extn: 9042

Food & Nutrition Journals

Katie Wilson

[email protected]

1-702-714-7001Extn: 9042

General Science

Andrea Jason

[email protected]

1-702-714-7001Extn: 9043

Genetics & Molecular Biology Journals

Anna Melissa

[email protected]

1-702-714-7001Extn: 9006

Immunology & Microbiology Journals

David Gorantl

[email protected]

1-702-714-7001Extn: 9014

Materials Science Journals

Rachle Green

[email protected]

1-702-714-7001Extn: 9039

Nursing & Health Care Journals

Stephanie Skinner

[email protected]

1-702-714-7001Extn: 9039

Medical Journals

Nimmi Anna

[email protected]

1-702-714-7001Extn: 9038

Neuroscience & Psychology Journals

Nathan T

[email protected]

1-702-714-7001Extn: 9041

Pharmaceutical Sciences Journals

Ann Jose

[email protected]

1-702-714-7001Extn: 9007

Social & Political Science Journals

Steve Harry

[email protected]

1-702-714-7001Extn: 9042

 
© 2008- 2018 OMICS International - Open Access Publisher. Best viewed in Mozilla Firefox | Google Chrome | Above IE 7.0 version