Design, synthesis and evaluation of flavonoid derivatives as potent AChE inhibitors

Sheng, Rong; Lin, Xiao; Zhang, Jing; Chol, Kim Sun; Huang, Wenhai; Yang, Bo; He, Qiaojun; Hu, Yongzhou

doi:10.1016/j.bmc.2009.07.072

Cited by 73 publications

(38 citation statements)

References 13 publications

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“…In the recent years, some research groups selected flavonoids and optimized their chemical structures to develop new anti-AD agents (Fig. 1, A A A A and B B B B' [8,9].…”

Section: Inmentioning

confidence: 99%

Design, synthesis and evaluation of 4-dimethylamine flavonoid derivatives as potential multifunctional anti-Alzheimer agents

Luo

Wang

Chen

et al. 2016

European Journal of Medicinal Chemistry

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“…In the recent years, some research groups selected flavonoids and optimized their chemical structures to develop new anti-AD agents (Fig. 1, A A A A and B B B B' [8,9].…”

Section: Inmentioning

confidence: 99%

Design, synthesis and evaluation of 4-dimethylamine flavonoid derivatives as potential multifunctional anti-Alzheimer agents

Luo

Wang

Chen

et al. 2016

European Journal of Medicinal Chemistry

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“…25 Especially, an AChE and MAO-B dual inhibitor ladostigil 26 designed by Youdim had been advanced into phase II clinical trial in 2011, which confirmed the rationality and feasibility of MTDLs strategy in the treatment of AD. In continuation of our research on the design and synthesis of indole and quinoxaline derivatives as MTDLs for AD therapy, [27][28][29] we explored a new series of 2-methoxy-phenyl dimethyl-carbamate derivatives as site-activated multitarget-directed compounds.…”

Section: Introductionmentioning

confidence: 99%

Design, synthesis and evaluation of rivastigmine and curcumin hybrids as site-activated multitarget-directed ligands for Alzheimer’s disease therapy

Peng

Tang

et al. 2014

Bioorganic & Medicinal Chemistry

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“…Macluraxanthone and quercetin derivatives were found to have very good inhibitory activity against the cholinesterase. 34 Several modified novel carbamates have been synthesized and have been tested in silico and in vitro and have been found to have very good AChE inhibitory activity. 35 Some novel compounds such as pyridopyrimidine, synthesized in vitro, Figure 2 Major targets in Alzheimer's disease therapy.…”

Section: Conventional Drug Target Network In Ad Acetylcholinesterasementioning

confidence: 99%

Current and novel therapeutic molecules and targets in Alzheimer's disease

Kumar

Nisha

Silakari

et al. 2016

Journal of the Formosan Medical Association

126

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Alzheimer's disease (AD) is a neurodegenerative disorder in which the death of brain cells causes memory loss and cognitive decline, i.e., dementia. The disease starts with mild symptoms and gradually becomes severe. AD is one of the leading causes of mortality worldwide. Several different hallmarks of the disease have been reported such as deposits of β-amyloid around neurons, hyperphosphorylated tau protein, oxidative stress, dyshomeostasis of bio-metals, low levels of acetylcholine, etc. AD is not simple to diagnose since there is no single diagnostic test for it. Pharmacotherapy for AD currently provides only symptomatic relief and mostly targets cognitive revival. Computational biology approaches have proved to be reliable tools for the selection of novel targets and therapeutic ligands. Molecular docking is a key tool in computer-assisted drug design and development. Docking has been utilized to perform virtual screening on large libraries of compounds, and propose structural hypotheses of how the ligands bind with the target with lead optimization. Another potential application of docking is optimization stages of the drug-discovery cycle. This review summarizes the known drug targets of AD, in vivo active agents against AD, state-of-the-art docking studies done in AD, and future prospects of the docking with particular emphasis on AD.

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Design, synthesis and evaluation of flavonoid derivatives as potent AChE inhibitors

Cited by 73 publications

References 13 publications

Design, synthesis and evaluation of 4-dimethylamine flavonoid derivatives as potential multifunctional anti-Alzheimer agents

Design, synthesis and evaluation of 4-dimethylamine flavonoid derivatives as potential multifunctional anti-Alzheimer agents

Design, synthesis and evaluation of rivastigmine and curcumin hybrids as site-activated multitarget-directed ligands for Alzheimer’s disease therapy

Current and novel therapeutic molecules and targets in Alzheimer's disease

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