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Triazinoindole analogs as potent inhibitors of α-glucosidase: synthesis, biological evaluation and molecular docking studies. 2015
Fazal Rahim, and
Khadim Ullah, and
Hayat Ullah, and
Abdul Wadood, and
Muhammad Taha, and
Ashfaq Ur Rehman, and
Imad uddin, and
Muhammad Ashraf, and
Ayesha Shaukat, and
Wajid Rehman, and
Shafqat Hussain, and
Khalid Mohammed Khan
Department of Chemistry, Hazara University, Mansehra 21120, Khyber Pukhtunkhwa, Pakistan. Electronic address: fazalstar@gmail.com.
A new series of triazinoindole analogs 1-11 were synthesized, characterized by EI-MS and (1)H NMR, evaluated for α-glucosidase inhibitory potential. All eleven (11) analogs showed different range of α-glucosidase inhibitory potential with IC50 value ranging between 2.46±0.008 and 312.79±0.06 μM when compared with the standard acarbose (IC50, 38.25±0.12 μM). Among the series, compounds 1, 3, 4, 5, 7, 8, and 11 showed excellent inhibitory potential with IC50 values 2.46±0.008, 37.78±0.05, 28.91±0.0, 38.12±0.04, 37.43±0.03, 36.89±0.06 and 37.11±0.05 μM respectively. All other compounds also showed good enzyme inhibition. The binding modes of these analogs were confirmed through molecular docking.
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