New Biscoumarin Derivatives as Potent α-Glucosidase Inhibitors: Synthesis, Biological Evaluation, Kinetic Analysis, and Docking Study

被引：39

作者：

Mohammadi-Khanaposhtani, Maryam ^{[1
]}

Yahyavi, Hoda ^{[2
]}

Barzegaric, Ebrahim ^{[3
]}

Imanparast, Somaye ^{[4
,5
]}

Heravi, Majid M. ^{[2
]}

Faramarzi, Mohammad Ali ^{[4
,5
]}

Foroumadi, Alireza ^{[6
,7
]}

Adibi, Hossein ^{[8
]}

Larijani, Bagher ^{[8
]}

Mandavi, Mohammad ^{[8
]}

机构：

[1] Babol Univ Med Sci, Cellular & Mol Biol Res Ctr, Hlth Res Inst, Babol, Iran

[2] Alzahra Univ, Fac Chem & Phys, Dept Chem, Tehran, Iran

[3] Kermanshah Univ Med Sci, Med Biol Res Ctr, Kermanshah, Iran

[4] Univ Tehran Med Sci, Dept Pharmaceut Biotechnol, Fac Pharm, Tehran, Iran

[5] Univ Tehran Med Sci, Biotechnol Res Ctr, Tehran, Iran

[6] Univ Tehran Med Sci, Fac Pharm, Dept Med Chem, Tehran, Iran

[7] Univ Tehran Med Sci, Pharmaceut Sci Res Ctr, Tehran, Iran

[8] Univ Tehran Med Sci, Endocrinol & Metab Res Ctr, Endocrinol & Metab Clin Sci Inst, Tehran, Iran

来源：

POLYCYCLIC AROMATIC COMPOUNDS | 2020年 / 40卷 / 04期

关键词：

alpha-Glucosidase; biscoumarin; docking study; type; 2; diabetes; IN-VITRO EVALUATION; MOLECULAR DOCKING; DESIGN; COUMARINS; VIRUS; MODEL;

D O I：

10.1080/10406638.2018.1509359

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A new series of biscoumarin derivatives3a-nwere synthesized and evaluated for their alpha-glucosidase inhibitory activities. The reaction of the 4-aminocoumarin with benzaldehyde derivatives led to the formation of the title compounds in good yields. All the synthesized compounds showed potent alpha-glucosidase inhibitory activity with IC(50)ranging from 20.0 +/- 0.7 to180.1 +/- 0.8 mu M, in comparison with acarbose as the standard drug (IC50= 750.0 1.5 mu M). Among the synthesized compounds, 3,3'-(p-tolylmethylene)bis(4-amino-2H-chromen-2-one)3cwas found to be the most active compound with an IC(50)value of 20.0 +/- 0.7 mu M. Kinetic study exhibited that compound3cwas a competitive inhibitor against alpha-glucosidase (K-i= 22.4 mu M). In silico docking study for the most potent compound3cwas also performed.

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收藏

页码：915 / 926

页数：12

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