Quinoxaline Derivatives: Novel and Selective Butyrylcholinesterase Inhibitors

ISSN: 1875-6638 (Online)
ISSN: 1573-4064 (Print)


Volume 10, 8 Issues, 2014


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Medicinal Chemistry

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Quinoxaline Derivatives: Novel and Selective Butyrylcholinesterase Inhibitors

Author(s): Aurang Zeb, Abdul Hameed, Latifullah Khan, Imran Khan, Kourosh Dalvandi and M. Iqbal Choudhary

Affiliation: H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan

Abstract

Alzheimer's disease (AD) is a progressive brain disorder which occurs due to lower level of acetylcholine (ACh) neurotransmitters, and results in a gradual decline in memory and other cognitive processes. Acetycholinesterase (AChE) and butyrylcholinesterase (BChE) are considered to be primary regulators of the ACh level in brain. Evidence showed that AChE activity decreases in AD, while activity of BChE doesn’t change or even elevate in advanced AD, which suggests a key involvement of BChE in ACh hydrolysis during AD symptoms. Therefore, inhibiting the activity of BChE may be an effective way to control AD associated disorders. In this regard, a series of quinoxaline derivatives 1-17 was synthesized and biologically evaluated against cholinesterases (AChE and BChE) and as well as against a-chymotrypsin and urease. The compounds 1-17 were found to be selective inhibitor for BChE, as no activity was found against other enzymes. Among the series, compounds 6 (IC50 = 7.7 ± 1.0 μM) and 7 (IC50 = 9.7 ± 0.9 μM) were found to be the most active inhibitors against BChE. Their IC50 values are comparable to the standard, galantamine (IC50 = 6.6 ± 0.38 µM). Their considerable BChE inhibitory activity, make them selective candidates for the development of BChE inhibitors. Structure-activity relationship (SAR) of this new class of selective BChE inhibitors has been discussed


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Article Details

Volume: 10
First Page: 1
Last Page: 1
Page Count: 1
DOI: 10.2174/1573406410666140526145429
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