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

Autor: Chigurupati, Sridevi, Selvaraj, Manikandan, Mani, Vasudevan, Mohammad, Jahidul I., Selvarajan, Kesavanarayanan K., Akhtar, Shaikh S., Marikannan, Maharajan, Raj, Suthakaran, Teh, Lay K., Salleh, Mohd Z.
Zdroj: Medicinal Chemistry Research; Mar2018, Vol. 27 Issue 3, p807-816, 10p
Abstrakt: 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 µM and 0.31 ± 0.03 µM respectively. The antioxidant activity of C1 in terms of DPPH and ABTS was found to be 16.22 ± 0.02 µM and 17.2 ± 0.02 µM, whereas V1 showed antioxidant activities at 14.07 ± 0.02 µM and 15.06 ± 0.03 µM respectively. In silico studies based on molecular docking and ADME predictions revealed the significance of azomethine derivatives as the potent anti-Alzheimer agents. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index