Molecular hybridization as a tool for designing multitarget drug candidates for complex diseases
V Ivasiv, C Albertini, AE Gonçalves… - Current Topics in …, 2019 - ingentaconnect.com
Molecular hybridization is a well-exploited medicinal chemistry strategy that aims to combine
two molecules (or parts of them) in a new, single chemical entity. Recently, it has been …
two molecules (or parts of them) in a new, single chemical entity. Recently, it has been …
[HTML][HTML] Alzheimer's disease pharmacotherapy in relation to cholinergic system involvement
GD Stanciu, A Luca, RN Rusu, V Bild… - Biomolecules, 2019 - mdpi.com
Alzheimer's disease, a major and increasing global health challenge, is an irreversible,
progressive form of dementia, associated with an ongoing decline of brain functioning. The …
progressive form of dementia, associated with an ongoing decline of brain functioning. The …
Donepezil-based multi-functional cholinesterase inhibitors for treatment of Alzheimer's disease
Q Li, S He, Y Chen, F Feng, W Qu, H Sun - European journal of medicinal …, 2018 - Elsevier
Alzheimer's disease (AD) is one of the most common neurodegenerative disorders in elderly
people. Considering the multifactorial nature of AD, the concept of multi-target-directed …
people. Considering the multifactorial nature of AD, the concept of multi-target-directed …
Oxidative stress in Alzheimer's disease: are we connecting the dots? Miniperspective
M Rosini, E Simoni, A Milelli, A Minarini… - Journal of medicinal …, 2014 - ACS Publications
Redox impairment is a prominent feature of Alzheimer's disease (AD). It has led to the
“oxidative stress hypothesis”, which proposes antioxidants as beneficial therapeutic tools in …
“oxidative stress hypothesis”, which proposes antioxidants as beneficial therapeutic tools in …
Multitarget drug design strategy: quinone–tacrine hybrids designed to block amyloid-β aggregation and to exert anticholinesterase and antioxidant effects
E Nepovimova, E Uliassi, J Korabecny… - Journal of medicinal …, 2014 - ACS Publications
We report the identification of multitarget anti-Alzheimer compounds designed by combining
a naphthoquinone function and a tacrine fragment. In vitro, 15 compounds displayed …
a naphthoquinone function and a tacrine fragment. In vitro, 15 compounds displayed …
Tacrine derivatives and Alzheimer's disease
V Tumiatti, A Minarini, ML Bolognesi… - Current medicinal …, 2010 - ingentaconnect.com
To date, the pharmacotherapy of Alzheimer's disease (AD) has relied on
acetylcholinesterase (AChE) inhibitors (AChEIs) and, more recently, an N-methyl-D …
acetylcholinesterase (AChE) inhibitors (AChEIs) and, more recently, an N-methyl-D …
Tacrine–trolox hybrids: a novel class of centrally active, nonhepatotoxic multi-target-directed ligands exerting anticholinesterase and antioxidant activities with low in …
E Nepovimova, J Korabecny, R Dolezal… - Journal of Medicinal …, 2015 - ACS Publications
Coupling of two distinct pharmacophores, tacrine and trolox, endowed with different
biological properties, afforded 21 hybrid compounds as novel multifunctional candidates …
biological properties, afforded 21 hybrid compounds as novel multifunctional candidates …
Discovery and biological evaluation of a novel highly potent selective butyrylcholinsterase inhibitor
Q Li, S Xing, Y Chen, Q Liao, B Xiong… - Journal of Medicinal …, 2020 - ACS Publications
To discover novel BChE inhibitors, a hierarchical virtual screening protocol followed by
biochemical evaluation was applied. The most potent compound 8012-9656 (eq BChE …
biochemical evaluation was applied. The most potent compound 8012-9656 (eq BChE …
Novel Multitarget-Directed Ligands (MTDLs) with Acetylcholinesterase (AChE) Inhibitory and Serotonergic Subtype 4 Receptor (5-HT4R) Agonist Activities As …
C Rochais, C Lecoutey, F Gaven… - Journal of medicinal …, 2015 - ACS Publications
In this work, we describe the synthesis and in vitro evaluation of a novel series of multitarget-
directed ligands (MTDL) displaying both nanomolar dual-binding site (DBS) …
directed ligands (MTDL) displaying both nanomolar dual-binding site (DBS) …
Multi-target-directed cinnamic acid hybrids targeting Alzheimer's disease
A Drakontaeidi, E Pontiki - International journal of molecular sciences, 2024 - mdpi.com
Progressive cognitive decline in Alzheimer's disease (AD) is a growing challenge. Present
therapies are based on acetylcholinesterase inhibition providing only temporary relief …
therapies are based on acetylcholinesterase inhibition providing only temporary relief …