Version 1
: Received: 28 November 2019 / Approved: 29 November 2019 / Online: 29 November 2019 (10:28:22 CET)
How to cite:
Taha, M.; Rahim, F.; Hayat, S.; Selvaraj, M.; Farooq, R.K.; Ali Shah, S.A.; Zakaria, Z.A. Synthesis of Diabetic II Inhibitors Based on 2-mercaptobenzimidazole and their Molecular Docking Study. Preprints2019, 2019110375. https://doi.org/10.20944/preprints201911.0375.v1.
Taha, M.; Rahim, F.; Hayat, S.; Selvaraj, M.; Farooq, R.K.; Ali Shah, S.A.; Zakaria, Z.A. Synthesis of Diabetic II Inhibitors Based on 2-mercaptobenzimidazole and their Molecular Docking Study. Preprints 2019, 2019110375. https://doi.org/10.20944/preprints201911.0375.v1.
Cite as:
Taha, M.; Rahim, F.; Hayat, S.; Selvaraj, M.; Farooq, R.K.; Ali Shah, S.A.; Zakaria, Z.A. Synthesis of Diabetic II Inhibitors Based on 2-mercaptobenzimidazole and their Molecular Docking Study. Preprints2019, 2019110375. https://doi.org/10.20944/preprints201911.0375.v1.
Taha, M.; Rahim, F.; Hayat, S.; Selvaraj, M.; Farooq, R.K.; Ali Shah, S.A.; Zakaria, Z.A. Synthesis of Diabetic II Inhibitors Based on 2-mercaptobenzimidazole and their Molecular Docking Study. Preprints 2019, 2019110375. https://doi.org/10.20944/preprints201911.0375.v1.
Abstract
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.
Keywords
synthesis; 2-mercaptabezimidazole; sulfonamide; molecular docking study; α-amylase; sa
Subject
CHEMISTRY, Medicinal Chemistry
Copyright:
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
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