作者: Guangcheng Wang , Jing Wang , Zhenzhen Xie , Ming Chen , Luyao Li
DOI: 10.1016/J.BIOORG.2017.05.006
关键词: Acarbose 、 In vitro 、 Hydrogen bond 、 Oxindole 、 Stereochemistry 、 Active site 、 Indole test 、 Chemistry 、 Hydrophobic effect 、 Enzyme
摘要: Abstract 3,3-Di(indolyl)indolin-2-ones 4a - 4n were synthesized and evaluated for their in vitro α-glucosidase inhibitory activity. These newly compounds showed moderate to potent activity with IC 50 range from 5.98 ± 0.11 145.95 ± 0.46 μM, when compared the standard drug acarbose. Among this series of 3,3-di(indolyl)indolin-2-ones, compound 4j (5.98 ± 0.11 μM) having a 2-fluorobenzyl group on indole ring was found be most active compound. Molecular docking studies that have high binding affinities site enzyme through hydrogen bonds, arene-cation, π-π stacking hydrophobic interactions. This study these 3,3-di(indolyl)indolin-2-ones as new class inhibitors.