Next Article in Journal
Chemical Composition, Antibacterial and Antifungal Activities of Crude Dittrichia viscosa (L.) Greuter Leaf Extracts
Next Article in Special Issue
Assessment of Enzyme Inhibition: A Review with Examples from the Development of Monoamine Oxidase and Cholinesterase Inhibitory Drugs
Previous Article in Journal
Metal Atom Effect on the Photophysical Properties of Mg(II), Zn(II), Cd(II), and Pd(II) Tetraphenylporphyrin Complexes Proposed as Possible Drugs in Photodynamic Therapy
Previous Article in Special Issue
Synthesis and Evaluation of Phenylxanthine Derivatives as Potential Dual A2AR Antagonists/MAO-B Inhibitors for Parkinson’s Disease
Article Menu
Issue 7 (July) cover image

Export Article

Open AccessArticle
Molecules 2017, 22(7), 1094; doi:10.3390/molecules22071094

Molecular Docking and Anticonvulsant Activity of Newly Synthesized Quinazoline Derivatives

1
Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia
2
Department of Pharmacognosy, College of Pharmacy, King Saud University, Riyadh 11495, Saudi Arabia
3
Department of Pharmacognosy, Faculty of Pharmacy, Helwan University, Cairo 11795, Egypt
4
Department of Chemistry, College of Science and Humanities, Prince Sattam bin Abdulaziz University, P.O. Box 83, Alkharj 11942, Saudi Arabia
5
Chemistry of Natural Products Group, Center of Excellence for Advanced Sciences, National Research Centre, Dokki, Cairo 12622, Egypt
6
Medicinal and Pharmaceutical Chemistry Department (Pharmacology group), Pharmaceutical and Drug Industries Research Division, National Research Centre, Dokki, Giza 12622, Egypt
*
Author to whom correspondence should be addressed.
Received: 29 April 2017 / Revised: 13 June 2017 / Accepted: 28 June 2017 / Published: 30 June 2017
(This article belongs to the Special Issue Polypharmacology and Multitarget Drug Discovery)
View Full-Text   |   Download PDF [3822 KB, uploaded 3 July 2017]   |  

Abstract

A new series of quinazoline-4(3H)-ones are evaluated for anticonvulsant activity. After intraperitoneal (ip) injection to albino mice at a dose of 100 mg/kg body weight, synthesized quinazolin-4(3H)-ones (1–24) were examined in the maximal electroshock (MES) induced seizures and subcutaneous pentylenetetrazole (scPTZ) induced seizure models in mice. The Rotarod method was applied to determine the neurotoxicity. Most of the compounds displayed anticonvulsant activity in the scPTZ screen at a dose range of 0.204–0.376 mmol/mL. Out of twenty-four, compounds 8, 13 and 19 proved to be the most active with a remarkable protection (100%) against PTZ induced convulsions and four times more potent activity than ethosuximide. The structure-activity relationship concluded valuable pharmacophoric information, which was confirmed by the molecular docking studies using the target enzyme human carbon anhydrase II (HCA II). The studied quinazoline analogues suggested that the butyl substitution at position 3 has a significant effect on preventing the spread of seizure discharge and on raising the seizure threshold. However, benzyl substitution at position 3 has shown a strong anticonvulsant activity but with less seizure prevention compared to the butyl substitution. View Full-Text
Keywords: quinazolines; anticonvulsant; phenobarbital; ethosuximide; molecular docking quinazolines; anticonvulsant; phenobarbital; ethosuximide; molecular docking
Figures

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

Scifeed alert for new publications

Never miss any articles matching your research from any publisher
  • Get alerts for new papers matching your research
  • Find out the new papers from selected authors
  • Updated daily for 49'000+ journals and 6000+ publishers
  • Define your Scifeed now

SciFeed Share & Cite This Article

MDPI and ACS Style

Abuelizz, H.A.; Dib, R.E.; Marzouk, M.; Anouar, E.-H.; A. Maklad, Y.; N. Attia, H.; Al-Salahi, R. Molecular Docking and Anticonvulsant Activity of Newly Synthesized Quinazoline Derivatives. Molecules 2017, 22, 1094.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]

Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top