Synthesis, antimicrobial and α-glucosidase inhibitory potential of mannich bases of mercapto oxadiazoles and their molecular docking studies

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Abstract

In the current study a series of eight Mannich bases were synthesized by incorporating 5-subsituted-1,3,4-oxadiazole-2-thione scaffold. The target compounds were evaluated for their antimicrobial and α-glucosidase inhibitory activity. All the synthesized Mannich bases exhibited α-glucosidase inhibitory activity with IC50 values between 43.05 ± 0.11 and 78.27 ± 0.44 when compared with standard acarbose 27.10 ± 0.51. Two compounds 3c and 4c containing morpholine moiety exhibited 85% & 82% inhibition as compared to the standard drug (acarbose) which gives 94% inhibition at dose level of 100 µg/mL. None of the compounds showed significant antimicrobial activity. The interactions of the all compounds with α-glucosidase enzyme were further studied with the help of docking analysis.

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Ahmad, S., Nadeem, H., Muhammad, S. A., Naz, S., Imran, M., & Saeed, A. (2018). Synthesis, antimicrobial and α-glucosidase inhibitory potential of mannich bases of mercapto oxadiazoles and their molecular docking studies. Farmacia, 66(4), 708–717. https://doi.org/10.31925/farmacia.2018.4.22

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