Abstract

IN-SILICO DESIGN AND SYNTHETIC STRATEGY OF BENZIMIDAZOLE-OXADIAZOLE SCAFFOLDS AS POTENT ANTIDIABETIC AGENTS

Ashitha Sivadas K.*, Dr. Byju K., Dr. Biju C. R. and Dr. G. Babu

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Abstract

Objective: To design and synthesize benzimidazole bearing 1,3,4 oxadiazole derivatives followed by their invitro evaluation as antidiabetic agents. Methods: In this study, in-silico screening were done and six derivatives were selected on the basis of docking. Their structures have been established on the basis of their spectral analysis (IR, NMR, MASS). Then compounds have been tested for their invitro alpha glucosidase inhibition and glucose uptake activity. Docking has been predicted using Schrodinger Maestro 13.3 software. Results: All the synthesized compounds were shown to exhibit significant alpha glucosidase inhibitory property when compared with standard drug acarbose. The samples show gradual increase in inhibition, when the sample concentration increased from 100 to 500 μg/ml. In glucose uptake assay, all the synthesized compounds showed enhancing the glucose uptake in L6 cells compared to untreated cells (Control). The glucose uptake was found to be increasing in concentration dependant manner also. The highest glucose uptake activity was shown by the sample at the concentration of 100μg/ml. Conclusion: According to the studies, it is observed that the synthesis and antidiabetic activities of benzimidazole-oxadiazole derivatives have been shown significant activity. In particular, compounds with electron withdrawing substituents were more potent. The newly synthesized compounds appears to be promising leads for future design for antidiabetic treatment.

Keywords: Benzimidazole, Oxadiazole, Anti-diabetic activity, In-silico studies, Invitro studies, ?- glucosidase, Glucose uptake.