2-Aryl benzimidazoles: Synthesis, In vitro α-amylase inhibitory activity, and molecular docking study

被引：54

作者：

Adegboye, Akande Akinsola ^{[1
]}

Khan, Khalid Mohammed ^{[2
,4
]}

Salar, Uzma ^{[2
]}

Aboaba, Sherifat Adeyinka ^{[1
]}

Kanwal ^{[2
]}

Chigurupati, Sridevi ^{[3
]}

Fatima, Itrat ^{[2
]}

Taha, Mohammad ^{[4
]}

Wadood, Abdul ^{[5
]}

Mohammad, Jahidul Isalm ^{[6
]}

Khan, Huma ^{[5
]}

Perveen, Shahnaz ^{[7
]}

机构：

[1] Univ Ibadan, Dept Chem, Ibadan, Nigeria

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

[3] AIMST Univ, Fac Pharm, Dept Pharmaceut Chem, Bedong 08100, Kedah, Malaysia

[4] Imam Abdulmhman Bin Faisal Univ, IRMC, Dept Clin Pharm, POB 1982, Dammam 31441, Saudi Arabia

[5] Abdul Wali Khan Univ, UCSS, Dept Biochem, Computat Med Chem Lab, Mardan, Pakistan

[6] CUCMS, Fac Med, Dept Pharmacol, Cyberjaya 63000, Malaysia

[7] PCSIR Labs Complex Karachi, Karachi 75280, Pakistan

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2018年 / 150卷

关键词：

Benzimidazole; alpha-Amylase; In vitro; In silico; Structure-activity relationship (SAR); DRUG SYNTHESIS BIODS; BIOLOGICAL-ACTIVITIES; DERIVATIVES; GLUCOSIDASE; SILICO; IMIDAZOLES; PYRIMIDINE; ANALOGS; ENZYMES; PLANT;

D O I：

10.1016/j.ejmech.2018.03.011

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Despite of many diverse biological activities exhibited by benzimidazole scaffold, it is rarely explored for the alpha-amylase inhibitory activity. For that purpose, 2-aryl benzimidazole derivatives 1-45 were synthesized and screened for in vitro alpha-amylase inhibitory activity. Structures of all synthetic compounds were deduced by various spectroscopic techniques. All compounds revealed inhibition potential with IC50 values of 1.48 +/- 038-2.99 +/- 0.14 mu M, when compared to the standard acarbose (IC50 = 1.46 +/- 0.26 mu M). Limited SAR suggested that the variation in the inhibitory activities of the compounds are the result of different substitutions on aryl ring. In order to rationalize the binding interactions of most active compounds with the active site of alpha-amylase enzyme, in silico study was conducted. (C) 2018 Elsevier Masson SAS. All rights reserved.

引用

页码：248 / 260

页数：13

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