DESIGN, SYNTHESIS, IN-SILICO STUDIES AND EVALUATION OF IN-VITRO ANTIDIABETIC ACTIVTY OF SOME NOVEL BENZIMIDAZOLE DERIVATIVES
AbstractNew Benzimidazole derivatives were designed and synthesized. To explain the activity of new derivatives, we have explored the binding affinity of the compounds against α-amylase (PDB ID: 4W93), the target enzyme for the antidiabetic activity. α-amylase is considered as primary target because it converts starch into maltose, which is followed by the production and transportation of the glucose into the blood. Docking study strongly enhanced the activity of these compounds as new discovered hits. The drug likeness score established the compounds to be pharmacokinetically active. All the reactions were monitored by TLC one spot technique, melting point analysis and the structures of the synthesized compounds were confirmed by UV, IR, proton NMR spectra. The inhibitory activity of all the derivatives against alpha amylase enzyme showed moderate activity in comparison to standard drug acarbose. Among all the derivatives, BM-1emerged with potent inhibitory activity. Compounds BM-2, BM-3 and BM-4 exhibited moderateinhibitoryactivity.BM-5was found to be the least potent derivative.
Article Information
14
2259-2266
1249 KB
33
English
IJPSR
K. P. Beena * and T. Akelesh
Department of Pharmaceutical Chemistry, Sri Ramakrishna Institute of Paramedical Sciences, College of Pharmacy, Coimbatore, Tamil Nadu, India.
beenaakelesh12@gmail.com
07 March 2025
19 March 2025
23 March 2025
10.13040/IJPSR.0975-8232.16(8).2259-66
01 August 2025
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