Discovery of huperzine A-tacrine hybrids as potent inhibitors of human cholinesterases targeting their midgorge recognition sites.

No abstract is available for this paper.

• Publication year

  2006

• Venue

  Journal of Medicinal Chemistry

• Publication date

  2006-05-04

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1021/JM060257TPMID 16722663
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• In vivo butyrylcholinesterase activity is not increased in Alzheimer's disease synapses

  2006cited by this paper
• Development of molecular probes for the identification of extra interaction sites in the mid-gorge and peripheral sites of butyrylcholinesterase (BuChE). Rational design of novel, selective, and highly potent BuChE inhibitors.

  2005cited by this paper
• Progress in clinical, pharmacological, chemical and structural biological studies of huperzine A: a drug of traditional chinese medicine origin for the treatment of Alzheimer's disease.

  2003cited by this paper
• Cholinergic function and Alzheimer's disease

  2003cited by this paper
• Specific targeting of acetylcholinesterase and butyrylcholinesterase recognition sites. Rational design of novel, selective, and highly potent cholinesterase inhibitors.

  2003cited by this paper
• Acetylcholinesterase knockouts establish central cholinergic pathways and can use butyrylcholinesterase to hydrolyze acetylcholine.

  2002cited by this paper
• Huprine X is a novel high-affinity inhibitor of acetylcholinesterase that is of interest for treatment of Alzheimer's disease.

  2000cited by this paper
• Potent, easily synthesized huperzine A-tacrine hybrid acetylcholinesterase inhibitors.

  1999cited by this paper
• Heterodimeric tacrine-based acetylcholinesterase inhibitors: investigating ligand-peripheral site interactions.

  1999cited by this paper
• Differences in active site gorge dimensions of cholinesterases revealed by binding of inhibitors to human butyrylcholinesterase.

  1997cited by this paper
• Highly Potent, Selective, and Low Cost Bis-tetrahydroaminacrine Inhibitors of Acetylcholinesterase

  1996cited by this paper

• Synthesis, Biological Evaluation, Molecular Docking, and In Silico ADME Predictions of Huperzine: A Derivative for the Novel Protective Application Against Neurodegenerations.

  2025cites this paper
• Biotechnological approaches for the production of neuroactive huperzine A.

  2025cites this paper
• Advances in the structural modification of Alzheimer's disease drug - Huperzine A.

  2024cites this paper
• Huperzine alkaloids: forty years of total syntheses.

  2023cites this paper
• Molecular docking and in vitro evaluation of a new hybrid molecule (JM-20) on cholinesterase activity from different sources.

  2019cites this paper
• Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018).

  2019cites this paper
• Structure-based virtual screening leading to discovery of highly selective butyrylcholinesterase inhibitors with solanaceous alkaloid scaffolds.

  2019cites this paper
• Tetrahydroquinoline-Isoxazole/Isoxazoline Hybrid Compounds as Potential Cholinesterases Inhibitors: Synthesis, Enzyme Inhibition Assays, and Molecular Modeling Studies

  2019cites this paper
• Phyto‐Tacrine Hybrids as Promising Drugs to Treat Alzheimer's Disease

  2019cites this paper
• Synthesis of 3-aminocoumarin-N-benzylpyridinium conjugates with nanomolar inhibitory activity against acetylcholinesterase

  2018cites this paper
• Running head: ANTITUMOR ACTIVITY OF NEW RITUXIMAB VARIANTS

  2017cites this paper
• On the use of the experimentally determined enzyme inhibition constant as a measure of absolute binding affinity

  2017cites this paper
• 5‐Amino‐6,7,8,9‐Tetrahydrobenzo[b][1,8]Naphthyridin‐2(1H)‐One: The first Example of a new Family of HuperTacrines for Alzheimer's Disease Therapy

  2017cites this paper
• Novel tacrine derivatives exhibiting improved acetylcholinesterase inhibition: Design, synthesis and biological evaluation.

  2017cites this paper
• Synthesis, Molecular Modeling, and Evaluation of Novel Sulfonylhydrazones as Acetylcholinesterase Inhibitors for Alzheimer's Disease

  2017cites this paper
• A review on tacrine-based scaffolds as multi-target drugs (MTDLs) for Alzheimer's disease.

  2017cites this paper
• Multiple Ligands in Neurodegenerative Diseases

  2017cites this paper
• AChE Inhibition-based Multi-target-directed Ligands, a Novel Pharmacological Approach for the Symptomatic and Disease-modifying Therapy of Alzheimer's Disease

  2016cites this paper
• Huperzine A from Huperzia serrata: a review of its sources, chemistry, pharmacology and toxicology

  2016cites this paper
• Nonuse of dental service by schoolchildren in Southern Brazil: impact of socioeconomics, behavioral and clinical factors

  2015cites this paper
• Direct- And Spacer-Coupled Codrug Strategies for the Treatment of Alzheimer’s Disease

  2015cites this paper
• Development of HuperTacrines as non-toxic, cholinesterase inhibitors for the potential treatment of Alzheimer's disease.

  2015cites this paper
• Combating HER2-overexpressing breast cancer through induction of calreticulin exposure by Tras-Permut CrossMab

  2015cites this paper
• Cognitive Enhancers (Nootropics). Part 2: Drugs Interacting with Enzymes. Update 2014

  2014cites this paper
• Quinolone-benzylpiperidine derivatives as novel acetylcholinesterase inhibitor and antioxidant hybrids for Alzheimer disease.

  2014cites this paper
• Dual acting HIV inhibitors: integrated rational in silico design strategy

  2014cites this paper
• Discovery of novel 2,6-disubstituted pyridazinone derivatives as acetylcholinesterase inhibitors.

  2013cites this paper
• The multifactorial nature of Alzheimer's disease for developing potential therapeutics.

  2013cites this paper
• Synthesis of α-oxycarbanilinophosphonates and their anticholinesterase activities: the most potent derivative is bound to the peripheral site of acetylcholinesterase

  2013cites this paper
• Cognitive Enhancers (Nootropics). Part 2: Drugs Interacting with Enzymes

  2013cites this paper
• Design, synthesis and biological evaluation of coumarin alkylamines as potent and selective dual binding site inhibitors of acetylcholinesterase.

  2013cites this paper
• Predictions of BuChE Inhibitors Using Support Vector Machine and Naive Bayesian Classification Techniques in Drug Discovery

  2013cites this paper
• Disseny, síntesi, avaluació farmacològica i modelatge molecular de nous inhibidors de l’acetilcolinesterasa de lloc d’unió dual

  2012cites this paper
• Alzheimer's disease: emerging trends in small molecule therapies.

  2011cites this paper
• A hydrazide linker strategy for heterobivalent compounds as ortho- and allosteric ligands of acetylcholine-binding proteins.

  2011cites this paper
• Synthesis of isotopically labelled [14C]ZT‐1 (Debio‐9902), [d3]ZT‐1 and (−)‐[d3]huperzine A, a new generation of acetylcholinesterase inhibitors

  2011cites this paper
• Design, Synthesis, and Biological Evaluation of Coumarin Derivatives Tethered to an Edrophonium‐like Fragment as Highly Potent and Selective Dual Binding Site Acetylcholinesterase Inhibitors

  2010cites this paper
• Tacrine derivatives and Alzheimer's disease.

  2010cites this paper
• Structural determinants of the multifunctional profile of dual binding site acetylcholinesterase inhibitors as anti-Alzheimer agents.

  2010cites this paper
• Characterization of a rituximab variant with potent antitumor activity against rituximab-resistant B-cell lymphoma.

  2009cites this paper
• Pyrano[3,2-c]quinoline-6-chlorotacrine hybrids as a novel family of acetylcholinesterase- and beta-amyloid-directed anti-Alzheimer compounds.

  2009cites this paper
• The Protein-Protein Interface Evolution Acts in a Similar Way to Antibody Affinity Maturation*

  2009cites this paper
• Design and synthesis of tacrine-ferulic acid hybrids as multi-potent anti-Alzheimer drug candidates.

  2008cites this paper
• NO-donating tacrine hybrid compounds improve scopolamine-induced cognition impairment and show less hepatotoxicity.

  2008cites this paper
• Homo- and hetero-bivalent edrophonium-like ammonium salts as highly potent, dual binding site AChE inhibitors.

  2008cites this paper
• Synthesis and biological evaluation of NO-donor-tacrine hybrids as hepatoprotective anti-Alzheimer drug candidates.

  2008cites this paper
• Exploiting protein fluctuations at the active-site gorge of human cholinesterases: further optimization of the design strategy to develop extremely potent inhibitors.

  2008cites this paper
• Acetylcholinesterase inhibitors as disease-modifying therapies for Alzheimer's disease.

  2008cites this paper
• Novel donepezil-based inhibitors of acetyl- and butyrylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation.

  2008cites this paper
• Rationally designed dual inhibitors of HIV reverse transcriptase and integrase.

  2007cites this paper
• Molecular hybridization: a useful tool in the design of new drug prototypes.

  2007cites this paper
• Bivalent ligands derived from Huperzine A as acetylcholinesterase inhibitors.

  2007cites this paper
• Recent developments in cholinesterases inhibitors for Alzheimer's disease treatment.

  2007cites this paper