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Triazinoindole analogs as potent inhibitors of α-glucosidase: synthesis, biological evaluation and molecular docking studies.

Abstract：

: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.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Rahim F,Ullah K,Ullah H,Wadood A,Taha M,Ur Rehman A,uddin I,Ashraf M,Shaukat A,Rehman W,Hussain S,Khan KM

doi

10.1016/j.bioorg.2014.12.001

subject

Has Abstract

pub_date

2015-02-01 00:00:00

pages

81-7

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(14)00127-8

journal_volume

58

pub_type

杂志文章

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