In search of new α-glucosidase inhibitors: Imidazolylpyrazole derivatives

被引：56

作者：

Chaudhry, Faryal ^{[1
,2
]}

Naureen, Sadia ^{[1
]}

Huma, Rahila ^{[2
]}

Shaukat, Ayesha ^{[3
]}

al-Rashida, Mariya ^{[4
]}

Asif, Nadia ^{[1
]}

Ashraf, Mohammad ^{[5
]}

Munawar, Munawar Ali ^{[1
]}

Khan, Misbahul Ain ^{[1
,5
]}

机构：

[1] Univ Punjab, Inst Chem, Lahore 54590, Pakistan

[2] Kinnaird Coll Women, Dept Chem, Lahore 54000, Pakistan

[3] Islamia Univ Bahawalpur, Dept Biochem & Biotechnol, Bahawalpur 63100, Pakistan

[4] Forman Christian Coll, Dept Chem, Ferozepur Rd, Lahore 54600, Pakistan

[5] Islamia Univ Bahawalpur, Dept Chem, Bahawalpur 63100, Pakistan

来源：

BIOORGANIC CHEMISTRY | 2017年 / 71卷

关键词：

Imidazolylpyrazoles; alpha-Glucosidase inhibition; Diabetes; Multicomponent reaction; Docking; BIOLOGICAL EVALUATION; DIABETES-MELLITUS; PYRAZOLE; POTENT; AGENTS; DISCOVERY; DESIGN; ANTIDEPRESSANT; THIOPHENE; MOIETY;

D O I：

10.1016/j.bioorg.2017.01.017

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Under three different reaction conditions (conventional heating, microwave irradiations and amino acid catalysis), a series of imidazolylpyrazoles (2a-2k) were synthesized in good to excellent yields from a mixture of three precursors: aryl(hetaryl) pyrazole-4-carbaldehydes (1a-1k), benzil and ammonium acetate. alpha-Glucosidase inhibition assay revealed a new class of highly potent agents wherein each compound displayed significant inhibitory potentials (in terms of percentage inhibition and relative IC50 values) as compared to that of the reference drug (Acarbose). Moreover, molecular modelling of most potent compounds 2h, 2j and 2k also helped in understanding the structure and activity relationship. (C) 2017 Elsevier Inc. All rights reserved.

引用

页码：102 / 109

页数：8

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