BackgroundThe 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).MethodsThe 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.ResultsThe 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.ConclusionThe 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.Graphical abstractCompound 24 superimposed with Ribavirin in CV B4 2A Proteinase enzyme (PDB: 1Z8R) active site.
From the leaves of Duranta repens (Verbenaceae) two new triterpene saponins, named durantanin IV (1) and V (2) were isolated. In addition, ten known compounds were isolated, namely a bidesmosidic saponin, oleanolic acid, three phenylethanoids and five flavonoids. All metabolites were isolated for the first time from this genus except for 3 (oleanolic acid) and 7 (E/Z acteoside). The structures were determined mainly by spectroscopic methods (UV, IR, HRESI-MS, 1H-, 13C-NMR, 1H-1H COSY, HSQC and HMBC). Cytotoxic screening of the chloroform, ethyl acetate and methanol extracts was carried out on brine shrimps. In addition, the investigated methanol extract and compounds 1, 2 and 7 showed significant cytotoxic activity against a HepG2 cell line.
Two New Flavonol Glycosides from Leaves of Koelreuteria paniculata.-Compounds (I) and (II) are isolated from dried leaves of Koelreuteria paniculata along with 9 known polyphenolic metabolites. -(MAHMOUD, I.; MOHARRAM, F. A.; MARZOUK, M. S.; SOLIMAN, H. S. M.; EL-DIB, R. A.; Pharmazie 56 (2001) 7, 580-582; Dep. Tanning and Protein
In spite of several studies of Stachys species, the literature lacks any information about the constituents of S. yemenensis Hedge. We report here the isolation of a new sesquiterpenetriol, stachytriol (1), along with the known compounds β-sitosterol (2), ursolic acid (3), penduletin (4), and benghalensin B (5). The structure elucidation of all isolated compounds was performed by extensive 1D and 2D NMR spectroscopic investigation.
Sablacaurin A and B, Two 19-nor-3,4-seco-Lanostane-Type Triterpenoids from Sabal causiarum and Sabal blackburniana, Respectively. -(EL-DIB, R.; KALOGA, M.; MAHMOUD, I.; SOLIMAN, H. S. M.; MOHARRAM, F. A.; KOLODZIEJ*, H.; Phytochemistry 65 (2004) 8, 1153-1157; Inst.
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