Synthesis of azomethines derived from cinnamaldehyde and vanillin: in vitro aetylcholinesterase inhibitory, antioxidant and insilico molecular docking studies

被引：40

作者：

Chigurupati, Sridevi ^{[1
]}

Selvaraj, Manikandan ^{[2
]}

Mani, Vasudevan ^{[3
]}

Mohammad, Jahidul I. ^{[4
]}

Selvarajan, Kesavanarayanan K. ^{[5
]}

Akhtar, Shaikh S. ^{[1
]}

Marikannan, Maharajan ^{[6
]}

Raj, Suthakaran ^{[7
]}

Teh, Lay K. ^{[2
,5
]}

Salleh, Mohd Z. ^{[2
,5
]}

机构：

[1] AIMST Univ, Fac Pharm, Bedong 08100, Kedah, Malaysia

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

[3] Qassim Univ, Dept Pharmacol & Toxicol, Coll Pharm, Buraydah 51452, Saudi Arabia

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

[5] Univ Hail, Dept Pharmacol & Toxicol, Coll Pharm, Hail 2440, Saudi Arabia

[6] Int Med Univ, Sch Pharm, Kuala Lumpur 57000, Malaysia

[7] Teegala Ram Reddy Coll Pharm, Dept Pharmaceut Chem, Fac Pharm, Hyderabad 500097, Andhra Pradesh, India

来源：

MEDICINAL CHEMISTRY RESEARCH | 2018年 / 27卷 / 03期

关键词：

Schiff bases; Cinnamaldehyde; Vanillin; Azomethines DPPH; Molecular docking; Acetylcholine esterase; SCHIFF-BASES; CHOLINESTERASE-INHIBITORS; DERIVATIVES; DISCOVERY;

D O I：

10.1007/s00044-017-2104-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In the present study, we report the synthesis of azomethines derived from cinnamaldehyde (C1-C3) and vanillin (V1-V3) using ethanol as a green solvent in the presence of triethyl amine. The synthesized compounds were characterized and investigated for their free radical scavenging activity and anti-Alzheimer properties by DPPH and acetylcholinesterase (AChE) inhibition assays. The anti-Alzheimer properties of the compounds were determined by molecular docking and ADME predictions. Compounds, C1 and V1 were found to be potential with IC50 values of 0.01 +/- 0.09 A mu M and 0.31 +/- 0.03 A mu M respectively. The antioxidant activity of C1 in terms of DPPH and ABTS was found to be 16.22 +/- 0.02 A mu M and 17.2 +/- 0.02 A mu M, whereas V1 showed antioxidant activities at 14.07 +/- 0.02 A mu M and 15.06 +/- 0.03 A mu M respectively. In silico studies based on molecular docking and ADME predictions revealed the significance of azomethine derivatives as the potent anti-Alzheimer agents.

引用

页码：807 / 816

页数：10

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