Benzoylquinazolinone derivatives as new potential antidiabetic agents: α-Glucosidase inhibition, kinetic, and docking studies

被引：8
|
作者：
Mohammadi-Khanaposhtani, Maryam [1 ]
Yahyavi, Hoda [2 ]
Imanparast, Somaye [3 ]
Harandi, Fereshte Nazemi [4 ]
Faramarzi, Mohammad Ali [3 ]
Foroumadi, Alireza [2 ]
Larijani, Bagher [5 ]
Biglar, Mahmood [5 ]
Mahdavi, Mohammad [5 ]
机构：
[1] Babol Univ Med Sci, Hlth Res Inst, Cellular & Mol Biol Res Ctr, Babol Sar, Iran
[2] Univ Tehran Med Sci, Fac Pharm & Pharmaceut Sci, Dept Med Chem, Res Ctr, Tehran, Iran
[3] Univ Tehran Med Sci, Fac Pharm & Biotechnol, Dept Pharmaceut Biotechnol, Res Ctr, Tehran, Iran
[4] Tarbiat Modares Univ, Chem Engn Dept, Biotechnol Grp, Tehran, Iran
[5] Univ Tehran Med Sci, Endocrinol & Metab Res Ctr, Endocrinol & Metab Clin Sci Inst, Tehran, Iran
来源：
JOURNAL OF THE CHINESE CHEMICAL SOCIETY | 2020年 / 67卷 / 05期
关键词：
antidiabetic; benzoylquinazolinone; kinetic analysis; alpha-glucosidase; QUINAZOLINONE DERIVATIVES; DESIGN; DISCOVERY;
D O I：
10.1002/jccs.201900268
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
Benzoylquinazolinone derivatives 3a-n were synthesized via a simple one-step reaction, and evaluated for in vitro alpha-glucosidase inhibitory activity. Compounds 3d, 3f-g, 3i, and 3m-n showed more inhibitory activity than standard drug acarbose (IC50 = 750.0 +/- 1.5 mu M), and among them, compound 3d displayed the highest alpha-glucosidase inhibitory activity (IC50 = 261.6 +/- 0.1 mu M). The kinetic analysis of the compound 3d revealed that this compound inhibited alpha-glucosidase in a competitive manner (K-i = 255 mu M). The docking studies were applied to predict binding modes of the synthesized compounds in active site of alpha-glucosidase.
引用
收藏
页码：856 / 863
页数：8
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