Synthesis of Diabetic II Inhibitors Based on 2-mercaptobenzimidazole and their Molecular Docking Study

Muhammad Taha; Fazal Rahim; Shawkat Hayat; Manikandan Selvaraj; Rai Khalid Farooq; Sayed Adnan Ali Shah; Zainul Amiruddin Zakaria

doi:10.20944/preprints201911.0375.v1

Preprint Article Version 1 This version is not peer-reviewed

Version 1 : Received: 28 November 2019 / Approved: 29 November 2019 / Online: 29 November 2019 (10:28:22 CET)

In the search of potent α-amylase inhibitors, we have synthesized seventeen derivatives of 2-mercaptobenzimidazole bearing sulfonamide (1-17) and evaluated for their α-amylase inhibitory potential. All compounds display a variable degree of α-amylase activity having IC50 values ranging between 0.90 ± 0.05 to 11.20 ± 0.30 µM when compared with the standard drug acarbose having IC50 value 1.70 ± 0.10 µM. Compound 1, 2, 11, 12 and 14 having IC50 values 1.40 ± 0.10, 1.30 ± 0.05, 0.90 ± 0.05, 1.60 ± 0.05 and 1.60 ± 0.10 µM respectively were found many folds better than the standard drug acarbose. The remaining analogs showed good inhibitory potentials. All the synthesized compounds were characterized by HREI-MS, 1H and 13C-NMR. Structure activity relationship (SAR) has been recognized for all newly synthesized analogs. Through molecular docking study, binding mode of active analogs with α-amylase enzyme was confirmed.

synthesis; 2-mercaptabezimidazole; sulfonamide; molecular docking study; α-amylase; sa

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Synthesis of Diabetic II Inhibitors Based on 2-mercaptobenzimidazole and their Molecular Docking Study

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