Synthesis and screening of some novel fused thiophene and thienopyrimidine derivatives for anti-avian influenza virus (H5N1) activity

Rashad, Aymn E.; Shamroukh, Ahmed H.; Abdel-Megeid, Randa E.; Mostafa, Ahmed; El-Shesheny, Rabeh; Kandeil, Ahmed; Ali, Mohammed Farid; Banert, Klaus

doi:10.1016/j.ejmech.2010.08.044

Cited by 94 publications

(56 citation statements)

References 22 publications

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“…Treatment of 5-amino-2-(p-tolylamino)-4-phenylthieno [2,3-d]pyrimidine-6-carbonitrile 7 with sodium azide and ammonium chloride in DMF, followed by acidification, afforded the corresponding 5-amino-2-(ptolylamino)-4-phenyl-6-(1H-tetrazol-5-yl)-thieno [2,3-d]pyrimidine (8). Aminotetrazolothienopyrimidine 8 was considered as precursor to the synthesis of other heterocyclic compounds, Thus, compound 8 was reacted with triethyl orthoformate in the presence of glacial acetic acid to afford the corresponding 9-p-tolylamino-7-phenyltetrazolo[1",5":1',6']pyrimido [4',5':4,5]thieno [2,3-d]pyrimidine (9). Compound 8 reacted with benzaldehyde in refluxing ethanol in the presence of a few drops of piperidine to afford 5,7-diphenyl-9-(p-tolylamino)-5,6-dihydrotetrazolo[1",5":1',6']pyrimido [4',5':4,5]thieno[2,3-d]pyrimidine 10.…”

Section: Resultsmentioning

confidence: 99%

“…Pyrimidine and thienopyrimidine derivatives display a broad variety of biological activities, such as anticancer, [1][2][3][4][5][6] antiviral, [7][8][9] antitumor, [10][11][12][13][14][15] anti-inflammatory, 16,17 antimicrobial, [18][19] antimalarial 20 and antioxidant activities. 21,22 Also thienopyrimidines have long been the subject of chemical and biological research.…”

Section: Introductionmentioning

confidence: 99%

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Synthesis and antimicrobial activity of some new thienopyrimidine derivatives

Tolba¹,

El‐Dean²,

Ahmed³

et al. 2017

Arkivoc

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Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Synthesis and antimicrobial activity of some new thienopyrimidine derivatives

Tolba¹,

El‐Dean²,

Ahmed³

et al. 2017

Arkivoc

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“…The cytotoxic effect of each sterol was tested individually in MadinDarby Canine kidney cells (MDCK) (friendly obtained from St. Jude Children's Research Hospital) using the 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT, Lonza) with minor modification as previously described [19]. Briefly, MDCK cells were seeded in 96 well culture plates and incubated for 24 h at 37 °C in 5% COR 2R.…”

Section: Cytotoxicity Assaymentioning

confidence: 99%

Sterols Bioactivity of Ruta Graveolens L. And Murraya Paniculata L.

Baker

Ibrahim

Kandeil

et al. 2017

Int J Pharm Pharm Sci

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Objective: Ruta graveolens L. (R. graveolens) and Murraya paniculata L. (M. paniculata) are medicinal plants belonging to Rutaceae family have many uses in traditional medicine. The aim of the present study was to investigate sterols bioactivity of the two Rutaceae plant leaves.Methods: Sterols of the two Rutaceae plant leaves were identified using GC/MS. The antioxidant activities of the sterols of these herbs were evaluated by three different methods; free radical scavenging using 2,2′-Azino-bis (3-ethylbenzthiazoline-6-sulfonic acid) (ABTS), 1,1-Diphenyl-2-picryl-hydrazyl ( Results: GC/MS assay showed β-Sitosterol (36%) as the most abundant sterols of R. graveolens followed by stigmasterol (18%), while stigmasterol (25.2%) was the most abundant one of M. paniculata steroids. The anti-inflammatory potential of R. graveolens steroids was significantly higher than that of diclofenac sodium (standard drug). M. paniculata sterols have higher antiviral activity (IC DPPH) and total antioxidant activity. The anticancer activity of the sterols was determined by MTT assay against colorectal cancer HCT116, breast cancer MCF7, liver cancer HepG2 and lung cancer A549 cell lines. Anti-inflammatory activity was evaluated using albumin denaturation assay and antiviral activities against H5N1 virus were carried out using plaque reduction assay. 50= 0.15 of µg/ml) than R. graveolens sterols (IC50 Conclusion:The current study suggests that the sterols of M. paniculata have more anti-viral activity than R. graveolens sterols which showed more anticancer and anti-inflammatory activities. = 7.8 of µg/ml). The sterols of R. graveolens showed anticancer activity against MCF7 and A549 cells with inhibition 84.3 and 81%, at 100 µg/ml respectively. While M. paniculata sterols showed 77.3% inhibition against A549 cells.

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“…New synthesized thiazolopyrimidine (TPYD) derivatives; hetero-cyclic compounds were found to possess a variety of pronounced activities such as anti-parkinsonism, hypoglycemic, antimicrobial activities [8] antiinflammatory, analgesic [9-10], anti-avian influenza virus (H5N1) [11], against herpes simplex virus type-1 (HSV-1) and hepatitis-A virus (HAV) [12], serotonin 5-HT 6 receptor antagonist [13]. Heterocyclic compounds were reported as inhibitors of glycogen synthase kinase-3(GSK-3) and potent anti-tumor agents [14][15].…”

Section: Introductionmentioning

confidence: 99%