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

页码：856 / 863

页数：8

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