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Synthesis and In Silico Docking Study towards M-Pro of Novel Heterocyclic Compounds Derived from Pyrazolopyrimidinone as Putative SARS-CoV-2 Inhibitors.
Horchani, Mabrouk; Heise, Niels V; Csuk, René; Ben Jannet, Hichem; Harrath, Abdel Halim; Romdhane, Anis.
Afiliación
  • Horchani M; Laboratory of Heterocyclic Chemistry, Natural Products and Reactivity, Medicinal Chemistry and Natural Products (LR11ES39), Faculty of Sciences of Monastir, University of Monastir, Monastir 5000, Tunisia.
  • Heise NV; Department of Organic Chemistry, Martin-Luther-University Halle-Wittenberg, Kurt-Mothes-Str. 2, D-06120 Halle, Germany.
  • Csuk R; Department of Organic Chemistry, Martin-Luther-University Halle-Wittenberg, Kurt-Mothes-Str. 2, D-06120 Halle, Germany.
  • Ben Jannet H; Laboratory of Heterocyclic Chemistry, Natural Products and Reactivity, Medicinal Chemistry and Natural Products (LR11ES39), Faculty of Sciences of Monastir, University of Monastir, Monastir 5000, Tunisia.
  • Harrath AH; Department of Zoology, College of Science, King Saud University, Riyad 11451, Saudi Arabia.
  • Romdhane A; Laboratory of Heterocyclic Chemistry, Natural Products and Reactivity, Medicinal Chemistry and Natural Products (LR11ES39), Faculty of Sciences of Monastir, University of Monastir, Monastir 5000, Tunisia.
Molecules ; 27(16)2022 Aug 19.
Article en En | MEDLINE | ID: mdl-36014537
In addition to vaccines, antiviral drugs are essential in order to suppress COVID-19. Although some inhibitor candidates have been determined to target the SARS-CoV-2 protein, there is still an urgent need to continue researching novel inhibitors of the SARS-CoV-2 main protease 'Omicron P132H', a protein that has recently been discovered. In the present study, in the search for therapeutic alternatives to treat COVID-19 and its recent variants, we conducted a structure-based virtual screening using docking studies for a new series of pyrazolo[3,4-d]pyrimidin-4(5H)-one derivatives 5-13, which were synthesized from the condensation reaction of pyrazolopyrimidinone-hydrazide (4) with a series of electrophiles. Some significant ADMET predictions-in addition to the docking results-were obtained based on the types of interactions formed and the binding energy values were compared to the reference anti- SARS-CoV-2 redocked drug nirmatrelvir.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Tratamiento Farmacológico de COVID-19 / Compuestos Heterocíclicos Límite: Humans Idioma: En Revista: Molecules Asunto de la revista: BIOLOGIA Año: 2022 Tipo del documento: Article País de afiliación: Túnez Pais de publicación: Suiza

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Tratamiento Farmacológico de COVID-19 / Compuestos Heterocíclicos Límite: Humans Idioma: En Revista: Molecules Asunto de la revista: BIOLOGIA Año: 2022 Tipo del documento: Article País de afiliación: Túnez Pais de publicación: Suiza