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      https://www.ias.ac.in/article/fulltext/jcsc/132/0100

    • Keywords

       

      quinazoline-2; 4-dione; a-amylase; a-glucosidase; Antioxidant; docking

    • Abstract

       

      The quinazoline-2,4-diones scaffold is found in bioactive compounds, commercial drugs and exhibit important biological activities. However, their antidiabetic activity is rarely explored. For this purpose, an easy one-pot three-components and straightforward synthesis of 3-substituted quinazoline-2,4-diones was designed, in both, the catalyst- and solvent-free conditions under microwave irradiation. Additionally, the synthesized compounds were screened for in vitro a-amylase and a-glucosidase inhibitory activity, as well as antioxidants and cytotoxicity. The quinazoline-2,4-diones were isolated, with yields in the range of 30-65%.The compounds 3d, 3e, 3g and 3h displayed moderate activity against a-amylase and/or a-glucosidase enzymes compared with the acarbose drug. The molecular docking study revealed that all active compounds displayed a different type of intermolecular interaction in the pocked site of these enzymes. Interestingly, inthe Artemia salina assay, the compound 3d exhibited a higher cytotoxic effect than 5-fluorouracil. All these results support the pharmacological potential of quinazoline-2,4-diones since all evaluated compounds behave as moderate inhibitors of the enzymes a-amylase and/or a-glucosidase.

    • Author Affiliations

       

      LUMADHAR SANTOS-BALLARDO1 FERNANDO GARCIA-PAEZ2 LORENZO A PICOSCORRALES1 ADRIAN OCHOA-TERAN3 PEDRO BASTIDAS4 LORANDA CALDERO NZAMORA5 GUADALUPE RENDON-MALDONADO1 ULISES OSUNA-MARTINEZ1 JUAN I SARMIENTO-SANCHEZ2

      1. Facultad de Ciencias Quı´mico-Biolo´gicas, Universidad Auto´noma de Sinaloa, Blvd. de las ame´ricas S/N, Campus Culiaca´n, 80040 Culiacan, Sinaloa, Mexico
      2. Facultad de Ingenierı´a Culiaca´n, Universidad Auto´noma de Sinaloa, Blvd. de las ame´ricas S/N, 80040 Culiaca´n, Sinaloa, Me´xico
      3. Tecnolo´gico Nacional de Me´xico / IT de Tijuana, Blvd. Alberto Limo´n Padilla S/N, Mesa de Otay, 22500 Tijuana, BC, Me´xico
      4. Laboratorio de Ana´lisis de Residuos de Plaguicidas, Centro de Investigacio´n en Alimentacio´n y Desarrollo A.C., Carretera a El Dorado Km 5.5, Campo El Diez, 80129 Culiaca´n, Sinaloa, Me´xico
      5. Facultad de Biologı´a, Universidad Auto´noma de Sinaloa, Blvd. de las ame´ricas S/N, Campus Culiaca´n, 80040 Culiaca´n, Sinaloa, Me´xico
    • Dates

       
  • Journal of Chemical Sciences | News

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