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

نویسندگان

چکیده

α-Glucosidase inhibition is considered as an effective strategy for the treatment of diabetes mellitus. Currently, three α-glucosidase inhibitors are being used drugs; Acarbose, Voglibose and Miglitol. The side effects these drugs forcing researchers to search new molecules. In this research work, novel 1,2,3-benzotriazin-4(3H)-one sulfonamides were synthesized investigated their activity. 2,4,6-Trichloro-1,3,5-triazine: N,N-dimethylformamide (TCT : DMF) adduct have been utilized direct synthesis targeted sulfonamides. All reactions performed at room temperature under mild conditions. In-vitro enzyme studies led us discover many potent demonstrating good excellent compound 5c with dimethyl substituent was found be a more inhibitor than acarbose IC50 value 29.75 ± 0.14 μM. Compounds 5a, 5b, 5d, 5e, 5f, 5m showed results 31.97 0.03, 33.24 0.01, 33.76 1.05, 35.98 30.87 0.51, 37.24 0.04 µM respectively. Further structure activity relationship analyzed by molecular docking studies.

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ژورنال

عنوان ژورنال: Medicinal Chemistry Research

سال: 2022

ISSN: ['1554-8120', '1054-2523']

DOI: https://doi.org/10.1007/s00044-022-02883-1