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 (doi: 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 (doi: 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 (doi: 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 (doi: 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.
Subject Areas
synthesis; 2-mercaptabezimidazole; sulfonamide; molecular docking study; α-amylase; sa
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.
Muhammad Taha
*
, 
, .png)