Synthesis and molecular docking studies of potent α-glucosidase inhibitors based on biscoumarin skeleton

被引：152

作者：

Khan, Khalid Mohammed ^{[1
]}

Rahim, Fazal ^{[2
]}

Wadood, Abdul ^{[3
]}

Kosar, Naveen ^{[2
]}

Taha, Muhammad ^{[4
,8
]}

Lalani, Salima ^{[1
]}

Khan, Aisha ^{[2
]}

Fakhri, Muhammad Imran ^{[1
]}

Junaid, Muhammad ^{[3
]}

Rehman, Wajid ^{[2
]}

Khan, Momin ^{[5
]}

Perveen, Shahnaz ^{[6
]}

Sajid, Muhammad ^{[7
]}

Choudhary, M. Iqbal ^{[1
]}

机构：

[1] Univ Karachi, Int Ctr Chem & Biol Sci, HEJ Res Inst Chem, Karachi 75270, Pakistan

[2] Hazara Univ, Dept Chem, Mansehra, Pakistan

[3] Abdul Wali Khan Univ, Dept Biochem, Computat Med Chem Lab, Mardan 23200, Pakistan

[4] Univ Teknol MARA UiTM, Atta Ur Rahman Inst Nat Prod Discovery, Bandar Puncak Alan 42300, Selangor, Malaysia

[5] Abdul Wali Khan Univ, Dept Chem, Mardan 23200, Pakistan

[6] PCSIR Labs Complex, Karachi 75280, Pakistan

[7] Hazara Univ, Dept Biochem, Mansehra, Pakistan

[8] Univ Tecknol MARA, Fac Sci Appl, Shah Alan 40450, Selangor, Malaysia

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2014年 / 81卷

关键词：

Biscoumarin; alpha-Glucosidase inhibition; Molecular docking; SCHIFF-BASES; VIRUS AGENTS; DERIVATIVES; COMPLEX; PROTEIN; SUGARS; NITROGEN; ACARBOSE; INSULIN; RATS;

D O I：

10.1016/j.ejmech.2014.05.010

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

In our effort directed toward the discovery of new anti-diabetic agent for the treatment of diabetes, a library of biscoumarin derivative 1-18 was synthesized and evaluated for alpha-glucosidase inhibitory potential. All eighteen (18) compounds displayed assorted alpha-glucosidase activity with IC50 values 16.5 -385.9 mu M, if compared with the standard acarbose (IC50 = 906 +/- 6.387 mu M). In addition, molecular docking studies were carried out to explore the binding interactions of biscoumarin derivatives with the enzyme. This study has identified a new class of potent alpha-glucosidase inhibitors. (C) 2014 Elsevier Masson SAS. All rights reserved.

引用

页码：245 / 252

页数：8

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