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ISSN: 2169-0138

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Research Article

Drug Design: An Efficient and Facile Synthesis of Novel Polar Benzimidazoles of Biological Interests

Yoon YK1*, Ali MA1, Wei AC1, Choon TS1 and Kumar RS2
1Institute for Research in Molecular Medicine, Universiti Sains Malaysia, Minden, 11800, Penang, Malaysia
2Department of Chemistry, College of Sciences, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia
Corresponding Author : Yoon YK
Institute for Research in Molecular Medicine
Universiti Sains Malaysia, Minden
11800, Penang, Malaysia
Tel no: +604 6593140
E-mail: [email protected]
Received October 25, 2013; Accepted November 29, 2013; Published December 06, 2013
Citation: Yoon YK, Ali MA, Wei AC, Choon TS, Kumar RS (2013) Drug Design: An Efficient and Facile Synthesis of Novel Polar Benzimidazoles of Biological Interests. Drug Des 3:110. doi:10.4172/2169-0138.1000110
Copyright: © 2013 Yoon YK, 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

A series of novel polar benzimidazoles were synthesized in a 4-step reaction starting from basic compound 4-fluoro-3-nitrobenzoic acid in good to excellent yield. The compounds generally fulfill the Lipinski’s rule of five to show their potential as drug lead compounds. The compounds were screened for their acetylcholinesterase (AChE) inhibitory activities and the most potent compound was found to be 5e which gave IC50 value of 31.04 μM. The structure of the novel polar benzimidazoles were characterized and confirmed by elemental and mass spectral analyses as well as 1H and 13C NMR spectroscopic data. All the compounds were found to be non-toxic when tested with VERO cells at 50 μM.

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