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Outcomes of Alzheimer's disease therapy with acetylcholinesterase inhibitors and memantine
TLDR
All currently available compounds for the management of AD are summarized, concentrating on clinical aspects such as the mechanisms of action, pharmacokinetics, pharmacodynamics and clinical trials, to provide perspective on current treatment options. Expand
7-MEOTA-donepezil like compounds as cholinesterase inhibitors: Synthesis, pharmacological evaluation, molecular modeling and QSAR studies.
TLDR
Overall, 7-MEOTA-donepezil like derivatives can be considered as interesting candidates for Alzheimer's disease treatment. Expand
Targeting copper(II)-induced oxidative stress and the acetylcholinesterase system in Alzheimer's disease using multifunctional tacrine-coumarin hybrid molecules.
TLDR
The results suggest that the design and investigation of multifunctional agents containing along with the acetylcholinesterase inhibitory segment also an antioxidant moiety capable of alleviating metal (copper)-induced oxidative stress, may be of importance in the treatment of Alzheimer's disease. Expand
Tacrine-Trolox Hybrids: A Novel Class of Centrally Active, Nonhepatotoxic Multi-Target-Directed Ligands Exerting Anticholinesterase and Antioxidant Activities with Low In Vivo Toxicity.
TLDR
Tacrine-trolox hybrids exhibited low in vivo toxicity after im administration in rats and potential to penetrate across blood-brain barrier and derivative 7u as the lead structure worthy of further investigation. Expand
Oximes: Inhibitors of Human Recombinant Acetylcholinesterase. A Structure-Activity Relationship (SAR) Study
TLDR
The goal of the present study is to determine how oxime structure influences the inhibition of human recombinant AChE (hrAChE), so 24 structurally different oximes were tested and the results compared to the previous eel A cholinesterase (EeA chE) experiments. Expand
Tacrine-resveratrol fused hybrids as multi-target-directed ligands against Alzheimer's disease.
TLDR
In a continuation of efforts aimed at a new series of anti-AD MTDLs, the structural features of the cholinesterase inhibitor drug tacrine are combined with that of resveratrol, which is known for its purported antioxidant and anti-neuroinflammatory activities. Expand
Synthesis and biological assessment of KojoTacrines as new agents for Alzheimer’s disease therapy
TLDR
The new MTSM KojoTacrines (KTs) were designed and synthesized by juxtaposition of selected pharmacophoric motifs from kojic acid and tacrine and KT2d was identified as less-hepatotoxic than tacrine, at higher concentration, a moderate, but selective human acetylcholinesterase inhibitor and an antioxidant agent. Expand
A resurrection of 7-MEOTA: a comparison with tacrine.
TLDR
Comparing these two cholinesterase inhibitors from various, mainly cholinergic, points of view relevant for a potential AD drug found that 7-MEOTA does not fall behind its more well-known parent compound - tacrine, and exerts better properties in most of the tests related to a possible AD treatment. Expand
The Antioxidant Additive Approach for Alzheimer's Disease Therapy: New Ferulic (Lipoic) Acid Plus Melatonin Modified Tacrines as Cholinesterases Inhibitors, Direct Antioxidants, and Nuclear Factor
TLDR
Compound 5c has been identified as a promising permeable agent showing excellent antioxidant properties, strong cholinesterase inhibitory activity, less hepatotoxicity than tacrine, and the best neuroprotective capacity, being able to significantly activate the Nrf2 transcriptional pathway. Expand
Design, Synthesis, and Biological Evaluation of 1-Benzylamino-2-hydroxyalkyl Derivatives as New Potential Disease-Modifying Multifunctional Anti-Alzheimer's Agents.
TLDR
A unique series of 1-benzylamino-2-hydroxyalkyl derivatives combining inhibitory activity against butyrylcholinesterase,β-secretase, β-amyloid, and tau protein aggregation, all related to mechanisms which underpin Alzheimer's disease are presented. Expand
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