تجاوز إلى المحتوى الرئيسي
User Image

Hatem A. Abuelizz

Professor

Professor of Medicinal Chemistry

كلية الصيدلة
College of Pharmacy- 2A128
المنشورات
مقال فى مجلة
2016

Molecular docking study and antiviral evaluation of 2-thioxo-benzo [g] quinazolin-4 (3H)-one derivatives

Marzouk, Rashad Al-Salahi, Hatem A Abuelizz, Hazem A Ghabbour, Rabab El-Dib, Mohamed . 2016

Background

The persistent appearance of viral strains that causes a resistant viral infection has led to continuous trials for the design and development of novel antiviral compounds. Benzoquinazoline compounds have been reported to exhibit an interesting antiviral activity. This work aims to study and evaluate the antiviral activity of a newly prepared 2-thioxo-benzo[g]quinazolin-4(3H)-one series against herpes simplex (HSV-1 & 2) and coxsackievirus (CVB4).

Methods

The antiviral activity was performed using the MTT assay, in which Vero cells (obtained from the American Type Culture Collection, ATCC) were propagated in fresh Dulbecco’s Modified Eagle’s Medium (DMEM) and challenged with 104 doses of the virus. Thereafter, the cultures were treated simultaneously with two-fold serial dilutions of the tested compound and incubated at 37 °C for 48 h. Molecular docking studies were done on the CVB4 2A proteinase enzyme using Molegro Virtual Docker software.

Results

The cytotoxicity (CC50), effective concentration (EC50) and the selectivity index (SI) values were determined. Based on their EC50 values, a number of the investigated compounds demonstrated weak to moderate activity relative to their parents. Accordingly, compounds 5–9, 11, 15–18, 21, 22, 24, 25, 27 and 28 were active against CVB4, and compounds 5 and 24 were active against HSV-1 and 2 in comparison to ribavirin and acyclovir, which were used as reference drugs.

Conclusion

The obtained results gave us some useful insights about the characteristic requirements for future trials to build up and design more active and selective antiviral 2-thioxo-benzo[g]quinazolin-4(3H)-one agents.

مجلة/صحيفة
Chemistry Central Journal
مزيد من المنشورات
publications

The pseudoglycosyltransferase (PsGT) VldE is a glycosyltransferase-like protein that is similar to trehalose 6-phosphate synthase (OtsA). However, in contrast to OtsA, which catalyzes condensation…

بواسطة Hatem A Abuelizz, Taifo Mahmud
2015
publications

The title compound, C18H20N4O2S2, is a new 1,3,4-oxa­diazole and a key pharmacophore of several biologically active agents. It is composed of a meth­yl(thio­phen-2-yl)-1,3,4-oxa­diazole-2(3H…

بواسطة Monirah A Al-Alshaikh, Hatem A Abuelizz, Ali A El-Emam, Mohammed SM Abdelbaky, Santiago Garcia-Granda
2016
publications

C31H36F2N6S, monoclinic, P21/c (no. 14), a = 14.7561(8) Å, b = 24.6766(13) Å, c = 7.7811(4) Å, β = 95.888(2)°, V = 2818.4(3) Å3, 

بواسطة Monirah A Al-Alshaikh, Hazem A Ghabbour, Hatem A Abuelizz, Obaid S Alruqi, Ali A El-Emam
2016