Synthesis and biological evaluation of indole derivatives as α-amylase inhibitor

被引：42

作者：

Imran, Syahrul ^{[1
,2
]}

Taha, Muhammad ^{[1
,2
]}

Selvaraj, Manikandan ^{[3
]}

Ismail, Nor Hadiani ^{[1
,2
]}

Chigurupati, Sridevi ^{[4
]}

Mohammad, Jahidul Islam ^{[5
]}

机构：

[1] Univ Teknol MARA UiTM, Atta Ur Rahman Inst Nat Prod Discovery, Puncak Alam Campus, Bandar Puncak Alam 42300, Selangor De, Malaysia

[2] UiTM Shah Alam, Fac Appl Sci, Shah Alam 40450, Selangor De, Malaysia

[3] Univ Teknol MARA UiTM, Integrat Pharmacogen Inst iPROMISE, Puncak Alam Campus, Bandar Puncak Alam 42300, Selangor Darul, Malaysia

[4] AIMST Univ, Fac Pharm, Dept Pharmaceut Chem, Semeling 08100, Bedong, Malaysia

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

来源：

BIOORGANIC CHEMISTRY | 2017年 / 73卷

关键词：

Synthesis; Indole; alpha-Amylase inhibitory potential; Molecular docking; SAR; GLUCOSIDASE INHIBITORS; POSTPRANDIAL HYPERGLYCEMIA; INSULIN GLARGINE; VARIABILITY; DISCOVERY; DOCKING; DETEMIR;

D O I：

10.1016/j.bioorg.2017.06.007

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：

A series of twenty indole hydrazone analogs (1-21) were synthesized, characterized by different spectroscopic techniques such as H-1 NMR and EI-MS, and screened for alpha-amylase inhibitory activity. All analogs showed a variable degree of alpha-amylase inhibition with IC50 values ranging between 1.66 and 2.65 mu M. Nine compounds that are 1 (2.23 +/- 0.01 mu M), 8 (2.44 +/- 0.12 mu M), 10 (1.92 +/- 0.12 mu M), 12 (2.49 +/- 0.17 mu M), 13 (1.66 +/- 0.09 mu M), 17 (2.25 +/- 0.1 mu M), 18 (1.87 +/- 0.25 mu M), 20 (1.83 +/- 0.63 mu M), and 19 (1.97 +/- 0.02 mu M) showed potent alpha-amylase inhibition when compared with the standard acarbose (1.05 +/- 0.29 mu M). Other analogs showed good to moderate alpha-amylase inhibition. The structure activity relationship is mainly focusing on difference of substituents on phenyl part. Molecular docking studies were carried out to understand the binding interaction of the most active compounds. (C) 2017 Elsevier Inc. All rights reserved.

引用

页码：121 / 127

页数：7

共 28 条

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