Romanian Society of Pharmaceutical Sciences

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SYNTHESIS, ANTIMICROBIAL AND α-GLUCOSIDASE INHIBITORY POTENTIAL OF MANNICH BASES OF MERCAPTO OXADIAZOLES AND THEIR MOLECULAR DOCKING STUDIES

SAKINA AHMAD 1, HUMAIRA NADEEM 1*, SYED AUN MUHAMMAD 2, SHAGUFTA NAZ 1, MUHAMMAD IMRAN 1, ADIL SAEED 1

1.Department of Pharmaceutical Chemistry, Riphah Institute of Pharmaceutical Sciences, Riphah International University, Islamabad, 7th Avenue, sector G-7/4, 44000, Islamabad, Pakistan
2.Department of Biotechnology, Bahauddin Zakariya University (BZU), Multan, Pakistan

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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.