Purpose: To evaluate the antibacterial, enzyme-inhibitory and hemolytic activities of Salkylated/
aralkylated 2-(1H-indol-3-ylmethyl)-1,3,4-oxadiazole-5-thiol derivatives.
Methods: Antibacterial activities of the compounds were evaluated using broth dilution method in 96
well plates. Enzyme inhibitory activities assays were investigated against α-glucosidase,
butyrylcholinesterase (BchE) and lipoxygenase (LOX) using acarbose, eserine and baicalien as
reference standards, respectively. A mixture of enzyme, test compound and the substrate was
incubated and variation in absorbance noted before and after incubation. In tests for hemolytic activities,
the compounds were incubated with red blood cells and variations in absorbance were used as indices
their hemolytic activities.
Results: The compounds were potent antibacterial agents. Five of them exhibited very good antibacterial
potential similar to ciprofloxacin, and had minimum inhibitory concentrations (MIC) of at least
9.00 ± 4.12 μM against
S. aureus
,
E.coli
, and
B. subtilis
. One of the compounds had strong enzyme
inhibitory potential against α-glucosidase, with IC
50 of 17.11 ± 0.02 μg/mL which was better than that of
standard acarbose (IC
50 38.25 ± 0.12 μg/mL). Another compound had 1.5 % hemolytic activity.
Conclusion: S-Alkylated/aralkylated 2-(1H-indol-3-ylmethyl)-1,3,4-oxadiazole-5-thiol deviratives with
valuable antibacterial, anti-enzymatic and hemolytic activities have been successfully synthesized.
These compounds may be useful in the development of pharmaceutical products.
