110 research outputs found

    Correction: El Azab, I.H., et al. Microwave-Assisted Synthesis of Novel 2H-Chromene Derivatives Bearing Phenylthiazolidinones and Their Biological Activity Assessment. Molecules 2014, 19, 19648-19664

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    The authors wish to revise the Author Affiliation section of the title paper, published in Molecules [1], (doi:10.3390/molecules191219648, website: http://www.mdpi.com/1420-3049/19/12/19648). To recognize the fact that the research described was performed in part at the facilities of Taif University and to acknowledge that institution’s generous financial support[...

    diazepine Based Heterocycles

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    An Efficient Synthetic Approach Towards Benzo[b]pyrano[2,3-e][1,4]diazepines, and Their Cytotoxic Activity

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    In search of unprecedented tri and/or tetrapod pharmacophoric conjugates, a series of 32 new 4-ethyl-1H-benzo[b][1,4]diazepin-2(3H)-ones were synthesized and properly elucidated using MS, IR, NMR, and elemental analysis. In vitro investigation of 11 compounds of this series, using a panel of two human tumor cell lines namely; human breast adenocarcinoma (MCF-7), and human colorectal carcinoma (HCT-116), revealed promising cytotoxic activities. Among all synthesized compounds, analogue 9 displayed maximum cytotoxicity with IC50 values of 16.19 ± 1.35 and 17.16 ± 1.54 μM against HCT-116 and MCF-7, respectively, compared to standard drug doxorubicin

    Design, Synthesis, and Antimicrobial Evaluation of New Annelated Pyrimido[2,1-c][1,2,4]triazolo[3,4-f][1,2,4]triazines

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    A series of 34 new pyrimido[2,1-c][1,2,4]triazine-3,4-diones were synthesized and fully characterized using IR, NMR, MS, and microanalytical analysis. In vitro investigation of 12 compounds of this series revealed promising antimicrobial activity of the conjugates 15a and 15f–j that were tagged with electron-withdrawing groups, with sensitivities ranging from 77% to as high as 100% of the positive control. The investigation of antimicrobial activity included Bacillus subtilis ATCC 6633, Staphylococcus aureus ATCC 6535, Pseudomonas aeruginosa ATCC 27853, and Escherichia coli ATCC 8739 (EC), and fungal strains Candida albicans ATCC 10231 and Aspergillus brasiliensis ATCC 16404

    Simple method for synthesis of isolated heterocyclic compounds incorporating 2-(2-bromoacetyl)isoindoline-1,3-dione and 2-(2-cyanoacetyl)isoindoline-1,3-dione

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    1194-12042-(2-Bromoacetyl)isoindoline-1,3-dione 2 and 2-(2-cyanoacetyl)isoindoline-1,3-dione 3 have been used as starting intermediates for synthesis of functionalized heterocyclic derivatives such as, 2-(2-aminothiazol-5-yl)isoindoline-1,3-dione 4, 2-(2-(benzylideneamino)thiazol-5-yl)isoindoline-1,3-dione 5, 2-(2-(3-chloro-2-oxo-4-phenylazetidin-1-yl)thiazol-5-yl)isoindoline-1,3-dione 6, 2-(2-(4-oxo-2-phenylthiazolidin-3-yl)thiazol-5-yl)isoindoline-1,3-dione 7, 2-(2-arylhydrazono)-2-bromo(cyano)acetyl)-isoindoline-1,3-dione 8, 6-bromo-5-(1,3-dioxoisoindolin-2-yl)-3-oxo-2-phenyl-2,3-dihydropyridazine- 4-carbonitrile 10a, 4-(1,3-dioxoisoindolin-2-yl)-6-oxo-1-phenyl-1,6-dihydropyridazine-3,5-dicarbonitrile 10b, 1-acetyl-3-(1,3-dioxoisoindolin-2-yl)-5-aryl-4,5-dihydro-1H-pyrazole-4-carbonitrile 12, 4-cyano-3-(1,3-dioxoisoindolin-2-yl)-5-aryl-4,5-dihydro-1H-pyrazole-1-carbothioamide 13, 3-(1,3-dioxoisoindolin-2-yl)-1-(4-oxo-4,5-dihydrothiazol-2-yl)-5-phenyl-4,5-dihydro-1H-pyrazole-4-carbonitrile 14, 3-(1,3-dioxoisoindolin-2-yl)-1-(5-(1,3-dioxoisoindolin-2-yl)thiazol-2-yl)-5-phenyl-4,5-dihydro-1H-pyrazole-4-carbonitrile 15, 2-(3-amino-5-(phenylamino)-1H-pyrazole-4-carbonyl)isoindoline-1,3-dione 17, 2-(5,7-dimethyl-2-(phenyl-amino)pyrazolo[1,5-a]pyrimidine-3-carbonyl)isoindoline-1,3-dione 18 and 2-(7-phenyl-2-(phenyl-amino)pyrazolo[1,5-a]pyrimidine-3-carbonyl)isoindoline-1,3-dione 20. The synthesized compounds have been characterized by IR, MS, 1H NMR and 13C NMR spectral analy­sis. </span

    Reactivity of β-enamino ester of benzo[f]chromene: One pot synthesis of isolated and heterocycle-fused derivatives of benzo[f] chromene

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    The formation of isolated and fused benzo[f]chromene derivatives was achieved via reacting ethyl 3-amino-1-phenyl-1H-benzo[f]chromene-2-carboxylate (1) with some selected reagents under basic conditions. The new compound, ethyl 3-(dimethylaminomethyleneamino)-1-phenyl-1H-benzo[f]chromene-2-carboxylate  (2) was prepared from compound 1 and N,N-dimethyl formamide in presence of phosphorus oxychloride under mild conditions in excellent yield using Vilsmeier reaction. Also, 10-amino-12-phenyl-9-sulfanyl-12H-benzo[f] chromeno[2,3-d]pyrimidine-11(10H)-one (12), 10-aryl-14-phenyl-14H-benzo[f]chromeno [2,3-d][1,3,4]thiadiazolo[3,2-a]pyrimidine-13-one (15), ethyl 3-(4-oxo-2-thioxothiazolidin-3-yl)-1-phenyl-1H-benzo[f]chromene-2-carboxylate (18), ethyl 3-(4-phenyl-2-thioxothiazol-3(2H)-yl)-1-phenyl-1H-benzo[f]chromene-2-carboxylate (20), ethyl 3-acetamido-1-phenyl-1H-benzo[f]chromene-2-carboxylate (21), and 10-amino-9-methyl-12-phenyl-12H-benzo[f] chromeno[2,3-d]pyrimidine-11(10H)-one (23) were prepared. The structures of these compounds were established by elemental analysis, IR, MS and NMR spectral analy­sis

    Microwave-Assisted Synthesis of Novel 2H-Chromene Derivatives Bearing Phenylthiazolidinones and Their Biological Activity Assessment

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    6-Hydroxy-2-oxo-2H-chromene-4-carbaldehyde (2), 6-chloro-2-oxo-2H-chromene-4-carbaldehyde (3) and 6-hydrazinyl-4-methyl-2H-chromen-2-one (5) were prepared as single-pharmacophore motif key intermediates. Compounds 2, 3 and 5 were incorporated in a series of multicomponent reactions (MCRs), under microwave assistance as well as conventional chemical synthesis processes, to afford a series of three and/or four-pharmacophoric-motif conjugates 8a,b, 11, 13, 16, 17, 19 and 20 in good yields. The newly synthesized compounds were characterized by IR, NMR, 13C-NMR, MS and elemental analyses. Finally the synthesized compounds have been screened for their biological activity whereupon they exhibited remarkable antimicrobial activity on different classes of bacteria and the fungus

    Azab Kaum Lūt Dalam Al-Qur’an (Kajian Kisah Berbasis Tafsir ‘Ilmī)

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    Thearchaeologicalfindings at Tall el-Hammam are often associated with evidence of a catastrophic event during the time of the Lūṭ\u27s destruction. The Qur\u27an describes this event as a warning to future generations, and the discoveries made can be correlated with the Qur\u27an and studied urgently. This qualitative research project utilized library research techniques to explore how the events described in the Qur\u27an can be discussed in scientific discourse. Three forms of doom are identified, including lightning sounds, earth turning, and stone rain, which can be researched through the scientific lens of mufasir \u27Ilmi. Some believe the event was caused by an erupting mountain, while others argue it was the result of a meteor shower. This study aims to demonstrate the relationship between scholarly interpretation and the scientific discoveries at Tall el-Hammam
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