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Design and synthesis of novel pyridazine N-aryl acetamides: In-vitro evaluation of α-glucosidase inhibition, docking, and kinetic studies.
Moghimi, Setareh; Toolabi, Mahsa; Salarinejad, Somayeh; Firoozpour, Loghman; Sadat Ebrahimi, Seyed Esmaeil; Safari, Fatemeh; Mojtabavi, Somayeh; Faramarzi, Mohammad Ali; Foroumadi, Alireza.
Afiliación
  • Moghimi S; Drug Design and Development Research Center, The Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medical Sciences, Tehran, Iran.
  • Toolabi M; Department of Medicinal Chemistry, School of Pharmacy, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran.
  • Salarinejad S; Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.
  • Firoozpour L; Drug Design and Development Research Center, The Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medical Sciences, Tehran, Iran.
  • Sadat Ebrahimi SE; Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.
  • Safari F; Department of Biology, Faculty of Science, University of Guilan, Rasht, Iran.
  • Mojtabavi S; Department of Pharmaceutical Biotechnology, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.
  • Faramarzi MA; Department of Pharmaceutical Biotechnology, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.
  • Foroumadi A; Drug Design and Development Research Center, The Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medical Sciences, Tehran, Iran; Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran. Electronic address: aforoumadi@yahoo.com.
Bioorg Chem ; 102: 104071, 2020 09.
Article en En | MEDLINE | ID: mdl-32688112
We herein applied the four step-synthetic route to prepare the pyridazine core attached to the various N-aryl acetamides. By this approach, a new series of pyridazine-based compounds were synthesized, characterized and evaluated for their activities against α-glucosidase enzyme. In-vitro α-glucosidase assay established that twelve compounds are more potent than acarbose. Compound 7a inhibited α-glucosidase with the IC50 value of 70.1 µM. The most potent compounds showed no cytotoxicity against HDF cell line. Molecular docking and kinetic studies were performed to determine the modes of interaction and inhibition, respectively.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Alfa-Glucosidasas / Simulación del Acoplamiento Molecular / Inhibidores de Glicósido Hidrolasas / Acetamidas Límite: Humans Idioma: En Revista: Bioorg Chem Año: 2020 Tipo del documento: Article País de afiliación: Irán Pais de publicación: Estados Unidos

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Alfa-Glucosidasas / Simulación del Acoplamiento Molecular / Inhibidores de Glicósido Hidrolasas / Acetamidas Límite: Humans Idioma: En Revista: Bioorg Chem Año: 2020 Tipo del documento: Article País de afiliación: Irán Pais de publicación: Estados Unidos