Medicinal Chemistry

Synthesis and Molecular Docking Study of Some New 4-{[4-(2-Furoyl)- 1-piperazinyl]methyl}-N-(substituted-phenyl)benzamides as Possible Therapeutic Entrants for Alzheimers Disease

Abstract

Ghulam Hussain, Muhammad Athar Abbasi, Aziz-ur- Rehman, Muhammad Ashraf, Aasia Noreen, Muhammad Arif Lodhi, Farman Ali Khan, Muhammad Shahid, Zahid Mushtaq and Syed Adnan Ali Shah

In the present work, a new series of different 4-{[4-(2-furoyl)-1-piperazinyl]methyl}-N-(substituted-phenyl) benzamides (5a-h) have been synthesized as possible therapeutic agents for the treatment of Alzheimer’s disease. The structural confirmation of all the synthesized compounds was carried out by their IR, 1H-NMR and EI-MS spectral data. Enzyme inhibition activity was performed against butyrylcholinestrase enzyme, which revealed that, 4-{[4-(2-furoyl)-1- piperazinyl]methyl}-N-(4-ethylphenyl)benzamide (5b) showed excellent IC50 value 0.82 ± 0.001 μM relative to Eserine, a reference standard having IC50 value of 0.85 ± 0.0001 μM. The enhanced potential of this molecule may be attributed to the 4-ethylphenyl group. As the cholinesterase enzyme inhibitors are good targets for Alzheimer’s disease, therefore, the inhibition study of these synthesized molecules was carried out to discover their possible therapeutic effect as target for aforesaid disease.