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Acyl pyrazole sulfonamides as new antidiabetic agents: synthesis, glucosidase inhibition studies, and molecular docking analysis.
Ahmed, Atteeque; Zaib, Sumera; Bhat, Mashooq Ahmad; Saeed, Aamer; Altaf, Muhammad Zain; Zahra, Fatima Tuz; Shabir, Ghulam; Rana, Nehal; Khan, Imtiaz.
Afiliación
  • Ahmed A; Department of Chemistry, Quaid-i-Azam University, Islamabad, Pakistan.
  • Zaib S; Department of Basic and Applied Chemistry, Faculty of Science and Technology, University of Central Punjab, Lahore, Pakistan.
  • Bhat MA; Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
  • Saeed A; Department of Chemistry, Quaid-i-Azam University, Islamabad, Pakistan.
  • Altaf MZ; Department of Basic and Applied Chemistry, Faculty of Science and Technology, University of Central Punjab, Lahore, Pakistan.
  • Zahra FT; Department of Chemistry, Quaid-i-Azam University, Islamabad, Pakistan.
  • Shabir G; Department of Chemistry, Quaid-i-Azam University, Islamabad, Pakistan.
  • Rana N; Department of Basic and Applied Chemistry, Faculty of Science and Technology, University of Central Punjab, Lahore, Pakistan.
  • Khan I; Department of Chemistry and Manchester Institute of Biotechnology, The University of Manchester, Manchester, United Kingdom.
Front Chem ; 12: 1380523, 2024.
Article en En | MEDLINE | ID: mdl-38694406
ABSTRACT
Diabetes mellitus is a multi-systematic chronic metabolic disorder and life-threatening disease resulting from impaired glucose homeostasis. The inhibition of glucosidase, particularly α-glucosidase, could serve as an effective methodology in treating diabetes. Attributed to the catalytic function of glucosidase, the present research focuses on the synthesis of sulfonamide-based acyl pyrazoles (5a-k) followed by their in vitro and in silico screening against α-glucosidase. The envisaged structures of prepared compounds were confirmed through NMR and FTIR spectroscopy and mass spectrometry. All compounds were found to be more potent against α-glucosidase than the standard drug, acarbose (IC50 = 35.1 ± 0.14 µM), with IC50 values ranging from 1.13 to 28.27 µM. However, compound 5a displayed the highest anti-diabetic activity (IC50 = 1.13 ± 0.06 µM). Furthermore, in silico studies revealed the intermolecular interactions of most potent compounds (5a and 5b), with active site residues reflecting the importance of pyrazole and sulfonamide moieties. This interaction pattern clearly manifests various structure-activity relationships, while the docking results correspond to the IC50 values of tested compounds. Hence, recent investigation reveals the medicinal significance of sulfonamide-clubbed pyrazole derivatives as prospective therapeutic candidates for treating type 2 diabetes mellitus (T2DM).
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: Front Chem Año: 2024 Tipo del documento: Article País de afiliación: Pakistán Pais de publicación: Suiza
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
Buscar en Google

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: Front Chem Año: 2024 Tipo del documento: Article País de afiliación: Pakistán Pais de publicación: Suiza