Triazinoindole analogs as potent inhibitors of α-glucosidase: Synthesis, biological evaluation and molecular docking studies
2014; Elsevier BV; Volume: 58; Linguagem: Inglês
10.1016/j.bioorg.2014.12.001
ISSN1090-2120
AutoresFazal Rahim, Khadim Ullah, Hayat Ullah, Abdul Wadood, Muhammad Taha, Ashfaq Ur Rehman, Imad Uddin, Muhammad Ashraf, Ayesha Shaukat, Wajid Rehman, Shafqat Hussain, Khalid Mohammed Khan,
Tópico(s)Diet, Metabolism, and Disease
ResumoA new series of triazinoindole analogs 1–11 were synthesized, characterized by EI-MS and 1H 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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