2018
DOI: 10.1038/s41598-018-22747-2
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Abstract: Alzheimer’s disease (AD) is a neurodegenerative disorder representing the leading cause of dementia and is affecting nearly 44 million people worldwide. AD is characterized by a progressive decline in acetylcholine levels in the cholinergic systems, which results in severe memory loss and cognitive impairments. Expression levels and activity of butyrylcholinesterase (BChE) enzyme has been noted to increase significantly in the late stages of AD, thus making it a viable drug target. A series of hydroxylated 2-p… Show more

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Cited by 77 publications
(54 citation statements)
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“…In molecular dynamics studies, compound 25 a expresses the best binding energy by showing interactions at the CAS and PAS of BuChE. Recently, a series of 2‐phenylbenzofuran derivatives with either two or three hydroxy substituents on the phenyl ring have been evaluated as selective inhibitors of BuChE . Among these derivatives, compounds 25 b and 25 c show maximum inhibitory activity against BuChE with IC 50 values of 6.23 and 3.57 μ m , respectively.…”
Section: Discussionmentioning
confidence: 99%
“…In molecular dynamics studies, compound 25 a expresses the best binding energy by showing interactions at the CAS and PAS of BuChE. Recently, a series of 2‐phenylbenzofuran derivatives with either two or three hydroxy substituents on the phenyl ring have been evaluated as selective inhibitors of BuChE . Among these derivatives, compounds 25 b and 25 c show maximum inhibitory activity against BuChE with IC 50 values of 6.23 and 3.57 μ m , respectively.…”
Section: Discussionmentioning
confidence: 99%
“…This class of chemical motifs have been shown to display antibacterial, antifungal, antioxidant, antitumoral, antiinflammatory, anticonvulsant, and anti-HIV bioactivities (Hiremathad et al, 2015;Khanam, 2015;Nevagi et al, 2015). Interestingly, benzofurans have also been found to have neuroprotective activity, inhibiting the important events involved in the AD process (Howlett et al, 1999;Allsop et al, 2001;Ono et al, 2002;Ono et al, 2006;Rizzo et al, 2008;Rizzo et al, 2012;Sashidhara et al, 2014;Ha et al, 2017;González-Ramírez et al, 2018;Kumar et al, 2018). Our research group has also investigated the role of natural fungal benzofurans in synaptic failure, decay of intracellular Ca 2+ transients and synaptic disorganization (González-Ramírez et al, 2018).…”
Section: Benzofuran Scaffolds Are Promising Targets To Explore the Nementioning
confidence: 99%
“…Thus, chemical probes containing benzofuran cores have yet to become approved drugs to control AD, mainly due to their modest potency. The lack of drug development could be attributed to the limited knowledge of protein-ligand interactions between benzofurans and important protein targets involved in AD progression (Howlett et al, 1999;Allsop et al, 2001;Kumar et al, 2018). In order to increase their efficacy, chemical transformation can be employed to tune their biological properties.…”
Section: Benzofuran Scaffolds Are Promising Targets To Explore the Nementioning
confidence: 99%
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“…Benzofurans find application in a variety of drugs and in other field of chemistry and agriculture [1]. Therefore, benzofuran derivatives are the important scaffold for drug discovery and possess broad spectrum biological activity like antimicrobial [2][3][4][5][6], anti-viral [7,8] anti-cancer [9][10][11][12][13][14][15][16], anti-Alzheimer [17][18][19][20], anti-hyperlipidemic [21], antinflammatory and anticonvulsivant [22], anti-tubercular [23], anti-pyretic [24] and protein tyrosine phosphatase inhibitors [25]. The benzofuran core is widely distributed in nature, mainly contained in products of secondary plant metabolism.…”
Section: Introductionmentioning
confidence: 99%