Design and Development of Multifunctional Hybrids of Ferulic Acid and 1,3,4-Oxadiazoles for the Treatment of Alzheimer’s Disease

Order of Publishing in Issue: 
Volume :14
Issue :1
January, 2020 - March, 2020
Page No: 
Avanish Tripathi#, Priyanka Kumari Choubey#, Ankit Seth, Piyoosh Sharma, Manish Kumar Tripathi and Sushant Kumar Shrivastava*
Department of Pharmaceutical Engineering & Technology, Indian Institute of Technology (Banaras Hindu University), Varanasi 221005, India

Ferulic acid-based multifunctional molecular hybrids of 1,3,4-oxadiazoles were designed, synthesized, and biologically evaluated for the treatment of Alzheimer’s disease. Among the synthesized compounds, the derivatives with 4- hydroxy-3,5-dimethoxy substituent (FA5 and CFA5) showed balanced inhibitory potential against hAChE, hBChE, and hBACE-1. Also, CFA5displayed remarkable PAS-AChE binding with significant displacement of propidium iodide, and appreciable blood-brain barrier permeability predictions in PAMPA-BBB assay. The thioflavin T assay in self- and AChE-induced experiments established the considerable anti-Aâ aggregatory activity of CFA5. Compound CFA5 also showed neuroprotective activity in Aâ-induced oxidative stress against SH-SY5Y neuroblastoma cell lines. Moreover, in vivo behavioral studies showed amelioration of cognitive dysfunction in rats tested by Y-maze. In silico molecular docking study showed consensual binding interactions of CFA5 with active binding site residues of AChE and BACE-1.

Alzheimer’s disease, Acetylcholinesterase (AChE), â-secretase-1 (BACE-1), Aâ aggregation, Molecular hybridization, Multifunctional agents.
PDF1.08 MB

To download full text articles and issues in PDF at no cost.All you have to do is fill out a brief registration form. It's easy and it's free. At any time, you may request removal of your contact information from our database.
Click here to Register | Click here if you have already registered

2018 ABAP Awards

Invitation for Nominations to 2019 ABAP Awards
The Association of Biotechnology and Pharmacy invites nominations for the following awards from the eligible talented people with proven track record and achievements on or before August 31, 2019 in the prescribed format.



Upcoming 0 events

  • No upcoming events available

User login