Antiviral activities of some synthesized methylsulfanyltriazoloquinazoline derivatives

Al‐Salahi, Rashad; Al-Omar, Mohamed A.; Alswaidan, Ibrahim A.; Marzouk, Mohamed; El‐Senousy, Waled M.; Amr, Abd El‐Galil E.

doi:10.1007/s11164-013-1177-1

Cited by 17 publications

(17 citation statements)

References 23 publications

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“…We previously reported our findings regarding the antiviral activity of isoquinazoline and triazoloquinazoline derivatives. The results suggested that quinazolines can be good platform for designing a new antiviral agent [ 11 – 13 ]. Here, we are reporting the results of an antiviral investigation for a new series of 2-thioxo-benzo[ g ]quinazolines 1 – 28 (Table 1 and Scheme 1 ) [ 18 ].…”

Section: Resultsmentioning

confidence: 99%

“…Recently, we have reported the biological activity of some prepared triazoloquinazolines against herpes simplex (HSV-1 & 2) and CVB4. However, a number of these prepared compounds were found to possess remarkable and significant antiviral activity [ 11 – 13 ]. Furthermore, synthetic chemistry has shown that benzoquinazoline is a valuable precursor for elaborating many structurally diverse bioactive molecules, particularly as influenza H5N1 and H1N1 antiviral agents [ 14 – 17 ].…”

Section: Introductionmentioning

confidence: 99%

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

Al‐Salahi

Abuelizz

Ghabbour

et al. 2016

Chemistry Central Journal

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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.

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Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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

Al‐Salahi

Abuelizz

Ghabbour

et al. 2016

Chemistry Central Journal

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“…Antimicrobial activities of the different time intervals released drugs (Doxorubicin, Chlorambucil and 5-fluorouracil) from prepared polymers were in vitro evaluated againsta panel of Gram positive [16] bacteria: Staphylococcus aureusATCC 29213, Bacillus subtilis ATCC6633; Gram negative bacteria: Escherichia coli ATCC, Pseudomonas aeruginosa AtCC27953 and fungi: Candida albicans NRRL y-47…”

Section: E-antimicrobial Activitymentioning

confidence: 99%

Assessment of the in vitro controlled release for some polymeric nanocomposites loaded with different drugs

et al. 2020

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S yNthesIzeD starch cellulose acetate coacrylate (SCACA)/ Sodium bentonite modified Tween-80 (MSB) nanocomposites holding anticancer drugs like 5-fluorouracil (5-FU), Doxorubicin hydrochloride (DOX), and Chlorambucil (CA) as controlled release systems were evaluated and assessment as antiproliferative activity towards breast cancer cell lines, and antimicrobial activity against some strains. the nanocomposites loaded drugs characterized by Zeta Potential, FTIR, SEM and TEM. The results indicated that no change in the chemical structures and physical properties of the drugs into the nanocomposites. the surface texture of the samples was homogenous and smooth with no evidence of aggregations after release and there were some pore like structure and cracks formed due to blooming of drug outside nanocomposites. the particle size diameter of the prepared polymer was found to be 73 ~ 79 nm. After holding Doxorubicin the particle size was from 18 to 24 nm , 5-fluorouracil from 15 to 18 nm and Chlorambucil was from 24 to 75 nm. the release of drug was measured spectrophotometrically. the values of drug released depend on the type and nature of drug as well as the environmental aqueous media. the release in alkaline and acidic media was more faster and higher than that in the neutral one. the invitro study results of anticancer drugs released from polymers placed inside the culture media, showed 5-FU was given an effective promising results compared to DOX and CA. The antimicrobial test revealed that, the released 5-FU gave the highest effect as antimicrobial against all tested strains followed by DOX and CA.

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“…Unambiguous conrmation of all products was nally achieved by clear identication of the 1 H and 13 C resonances of the accompanying functional groups or moieties, such as -SCH 3 , -SO 2 CH 3 , -OPh, benzyl, and phenethyl, and through comparison with data of structurally related compounds. [19][20][21][22][23][24]…”

Section: Chemistrymentioning

confidence: 99%

Synthesis and biological evaluation of 4-(1H-1,2,4-triazol-1-yl)benzoic acid hybrids as anticancer agents

et al. 2019

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Antiviral activities of some synthesized methylsulfanyltriazoloquinazoline derivatives

Cited by 17 publications

References 23 publications

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

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

Assessment of the in vitro controlled release for some polymeric nanocomposites loaded with different drugs

Synthesis and biological evaluation of 4-(1H-1,2,4-triazol-1-yl)benzoic acid hybrids as anticancer agents

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