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New Pyrazine Conjugates: Synthesis, Computational Studies, and Antiviral Properties against SARS-CoV-2
Faculty
Pharmacy
Year:
2021
Type of Publication:
ZU Hosted
Pages:
Authors:
Israa Abdallah Mostafa Sliem
Staff Zu Site
Abstract In Staff Site
Journal:
ChemMedChem Wiley
Volume:
Keywords :
, Pyrazine Conjugates: Synthesis, Computational Studies, , Antiviral
Abstract:
Currently, limited therapeutic options are available for severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2). We have developed a set of pyrazine-based small molecules. A series of pyrazine conjugates was synthesized by microwave-assisted click chemistry and benzotriazole chemistry. All the synthesized conjugates were screened against the SAR-CoV-2 virus and their cytotoxicity was determined. Computational studies were carried out to validate the biological data. Some of the pyrazine-triazole conjugates (5 d-g) and (S)-N-(1-(benzo[d]thiazol-2-yl)-2-phenylethyl)pyrazine-2-carboxamide 12 i show significant potency against SARS-CoV-2 among the synthesized conjugates. The selectivity index (SI) of potent conjugates indicates significant efficacy compared to the reference drug (Favipiravir).
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Israa Abdallah Mostafa Sliem, "An Efficient Greener Approach for N-Acylation of Amines in Water Using Benzotriazole Chemistry", Mdpi, 2020
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Department Related Publications
Etedaal Hassan Mohamed Abdulaal, "18. In situ annelation of enaminones by reaction with methyleneiminium intermediates", لايوجد, 1900
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Hanan Abdelraziek Abdelfattah Ali Hamied, "synthesis of some new imidazolones of expected antimicrobial activity", لايوجد, 1900
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Azza Mohamed Kadry , "35. Synthesis and potentiometric study of some dioxadiaza ionophores in ion selective electrodes", لايوجد, 1900
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Azza Mohamed Kadry , "16. Chemistry of quinazolines: Reinvestigation of the action of hydrazine on thioxo derivatives", لايوجد, 1900
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Azza Mohamed Kadry , "2. Reaction and rearrangement of 2,4-quinazolinediones", لايوجد, 1900
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