alexa Synthesis and Molecular Docking Study of Some New 4-{[4
ISSN: 2161-0444

Medicinal chemistry
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Research Article

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

Ghulam Hussain1, Muhammad Athar Abbasi1*, Aziz-ur-Rehman1, Sabahat Zahra Siddiqui1, Muhammad Ashraf2, Aasia Noreen2, Muhammad Arif Lodhi3, Farman Ali Khan3, Muhammad Shahid4, Zahid Mushtaq4 and Syed Adnan Ali Shah5,6

1Department of Chemistry, Government College University, Lahore-54000, Pakistan

2Department of Chemistry, The Islamia University of Bahawalpur, Bahawalpur-63100, Pakistan

3Department of Biochemistry, Abdul Wali Khan University, Mardan-23200, Pakistan

4Department of Biochemistry, University of Agriculture, Faisalabad-38040, Pakistan

5Faculty of Pharmacy, Universiti Teknologi MARA, Puncak Alam Campus, 42300 Bandar Puncak Alam, Selangor Darul Ehsan, Malaysia

6Atta-ur-Rahman Institute for Natural Products Discovery (AuRIns), Level 9, FF3, Universiti Teknologi MARA, Puncak Alam Campus, 42300 Bandar Puncak Alam, Selangor Darul Ehsan, Malaysia

*Corresponding Author:
Dr. Muhammad Athar Abbasi
Department of Chemistry, Government College
University, Lahore-54000, Pakistan
Tel: +92-42-111000010 extn. 266
E-mail: [email protected] [email protected]

Received date: February 16, 2016; Accepted date: February 27, 2016; Published date: February 29, 2016

Citation: Hussain G, Abbasi MA, Rehman A, Siddiqui SZ, Ashraf M, et al. (2016) Synthesis and Molecular Docking Study of Some New 4-{[4-(2-Furoyl)-1-piperazinyl]methyl}-N-(substituted-phenyl)benzamides as Possible Therapeutic Entrants for Alzheimer’s Disease. Med chem (Los Angeles) 6:129-136. doi:10.4172/2161-0444.1000337

Copyright: © 2016 Hussain G, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

 

Abstract

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.

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