Molecules (2019)
Update date:2022-08-04
Topics:
Taha, Muhammad
Alshamrani, Foziah J.
Rahim, Fazal
Hayat, Shawkat
Ullah, Hayat
Zaman, Khalid
Imran, Syahrul
Khan, Khalid Mohammed
Naz, Farzana
A new class of triazinoindole-bearing thiosemicarbazides (1-25) was synthesized and evaluated for α-glucosidase inhibitory potential. All synthesized analogs exhibited excellent inhibitory potential, with IC50 values ranging from 1.30 ± 0.01 to 35.80 ± 0.80 μM when compared to standard acarbose (an IC50 value of 38.60 ± 0.20 μM). Among the series, analogs 1 and 23 were found to be the most potent, with IC50 values of 1.30 ± 0.05 and 1.30 ± 0.01 μM, respectively. The structure- activity relationship (SAR) was mainly based upon bringing about different substituents on the phenyl rings. To confirm the binding interactions, a molecular docking study was performed.
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