Synthesis of 1,2,3-benzotriazin-4(3H)-one derivatives as α-glucosidase inhibitor and their in-silico study

Autor: Zunera Khalid, Syed Salman Shafqat, Hafiz Adnan Ahmad, Hafiz Muzzamil, Munawar Ali Munawar, Matloob Ahmad, Abdullah Mohammad Ahmad Asiri, Muhammad Ashraf
Rok vydání: 2022
Předmět:
Zdroj: Medicinal Chemistry Research. 31:819-831
ISSN: 1554-8120
1054-2523
DOI: 10.1007/s00044-022-02883-1
Popis: α-Glucosidase inhibition is considered as an effective strategy for the treatment of diabetes mellitus. Currently, three α-glucosidase inhibitors are being used as drugs; Acarbose, Voglibose and Miglitol. The side effects of these drugs are forcing researchers to search for new and effective molecules. In this research work, novel 1,2,3-benzotriazin-4(3H)-one sulfonamides were synthesized and investigated for their α-glucosidase inhibition activity. TCT: DMF adduct have been utilized for the direct synthesis of targeted sulfonamides. All reactions were performed at room temperature under mild conditions. In-vitro enzyme inhibition studies led us to discover many potent inhibitors demonstrating good to excellent activity. The compound 5c with dimethyl substituent was found to be more potent inhibitor than acarbose with the IC50 value of 29.75±0.14 μM. Compounds 5a, 5b, 5d, 5e, 5f and 5m showed good inhibition results with IC50 value 31.97±0.03, 33.24±0.01, 33.76±1.05, 35.98±0.03, 30.87±0.51 and 37.24±0.04 µM respectively. Further structure activity relationship was analyzed by molecular docking studies.
Databáze: OpenAIRE
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