125 articles for thisTarget
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Benzoflavones as cholesterol esterase inhibitors: Synthesis, biological evaluation and docking studies.
Guru Nanak Dev University
Aurone Mannich base derivatives as promising multifunctional agents with acetylcholinesterase inhibition, anti-ß-amyloid aggragation and neuroprotective properties for the treatment of Alzheimer's disease.
Sichuan University
Multitarget drug design strategy against Alzheimer's disease: Homoisoflavonoid Mannich base derivatives serve as acetylcholinesterase and monoamine oxidase B dual inhibitors with multifunctional properties.
Sichuan University
Design, synthesis and evaluation of rivastigmine and curcumin hybrids as site-activated multitarget-directed ligands for Alzheimer's disease therapy.
Zhejiang University
Potent reversible anticholinesterase agents. Bis- and mono-N-substituted benzoquinolinium halides.
TBA
Synthesis and insecticidal activity of novel carbamate derivatives as potential dual-binding site acetylcholinesterase inhibitors.
Chinese Academy of Agricultural Sciences
Use of ab initio calculations to predict the biological potency of carboxylesterase inhibitors.
University of California
Carbamate derivatives of indolines as cholinesterase inhibitors and antioxidants for the treatment of Alzheimer's disease.
Bar-Ilan University
Synthesis and evaluation of novel 4-[(3H,3aH,6aH)-3-phenyl)-4,6-dioxo-2-phenyldihydro-2H-pyrrolo[3,4-d]isoxazol-5(3H,6H,6aH)-yl]benzoic acid derivatives as potent acetylcholinesterase inhibitors and anti-amnestic agents.
Punjabi University
Synthesis of phenserine analogues and evaluation of their cholinesterase inhibitory activities.
Meiji Pharmaceutical University
Multipotent MAO and cholinesterase inhibitors for the treatment of Alzheimer's disease: synthesis, pharmacological analysis and molecular modeling of heterocyclic substituted alkyl and cycloalkyl propargyl amine.
Laboratorio De Radicales Libres Y Qu�Mica Computacional (Iqog, Csic)
Cholinestrase inhibitory effects of geranylated flavonoids from Paulownia tomentosa fruits.
Graduate School of Gyeongsang National University
Novel donepezil-based inhibitors of acetyl- and butyrylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation.
Laboratori De Qu�Mica Farmac�Utica (Unitat Associada Al Csic)
Exploiting protein fluctuations at the active-site gorge of human cholinesterases: further optimization of the design strategy to develop extremely potent inhibitors.
University of Siena
Design and synthesis of tacrine-ferulic acid hybrids as multi-potent anti-Alzheimer drug candidates.
Friedrich-Schiller-Universit£T Jena
Influence of sulfur oxidation state and steric bulk upon trifluoromethyl ketone (TFK) binding kinetics to carboxylesterases and fatty acid amide hydrolase (FAAH).
University of California
Brunneins A-C, beta-carboline alkaloids from Cortinarius brunneus.
Institute of Plant Biochemistry
Derivatives of oxoisoaporphine alkaloids: a novel class of selective acetylcholinesterase inhibitors.
Sun Yat-Sen University
Propidium-based polyamine ligands as potent inhibitors of acetylcholinesterase and acetylcholinesterase-induced amyloid-beta aggregation.
University of Bologna
Design, synthesis, and evaluation of 2-phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors.
Zhejiang University
Pyridophens: binary pyridostigmine-aprophen prodrugs with differential inhibition of acetylcholinesterase, butyrylcholinesterase, and muscarinic receptors.
Institute of Research
Synthesis and structure-activity relationships of acetylcholinesterase inhibitors: 1-benzyl-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine hydrochloride and related compounds.
Eisai
Synthesis and evaluation of 5-amino-5,6,7,8-tetrahydroquinolinones as potential agents for the treatment of Alzheimer's disease.
Hoechst-Roussel Pharmaceuticals
Potent, easily synthesized huperzine A-tacrine hybrid acetylcholinesterase inhibitors.
Hong Kong University of Science and Technology
Conformationally restricted carbamate inhibitors of horse serum butyrylcholinesterase.
National Chung-Hsing University
Benzenediol-berberine hybrids: multifunctional agents for Alzheimer's disease.
Guangzhou Institute of Biomedicine and Health
Formulating a new basis for the treatment against botulinum neurotoxin intoxication: 3,4-Diaminopyridine prodrug design and characterization.
The Scripps Research Institute
Homodimeric bis-quaternary heterocyclic ammonium salts as potent acetyl- and butyrylcholinesterase inhibitors: a systematic investigation of the influence of linker and cationic heads over affinity and selectivity.
Universidad De Granada
Design, synthesis and structure-activity relationship (SAR) studies of 2,4-disubstituted pyrimidine derivatives: dual activity as cholinesterase and A β-aggregation inhibitors.
University of Waterloo
Synthesis, biological evaluation and molecular modeling of novel triazole-containing berberine derivatives as acetylcholinesterase and β-amyloid aggregation inhibitors.
Sun Yat-Sen University
Design, synthesis and evaluation of novel tacrine-multialkoxybenzene hybrids as dual inhibitors for cholinesterases and amyloid beta aggregation.
Sun Yat-Sen University
Berberine derivatives, with substituted amino groups linked at the 9-position, as inhibitors of acetylcholinesterase/butyrylcholinesterase.
Sun Yat-Sen University
Multipotent drugs with cholinergic and neuroprotective properties for the treatment of Alzheimer and neuronal vascular diseases. I. Synthesis, biological assessment, and molecular modeling of simple and readily available 2-aminopyridine-, and 2-chloropyridine-3,5-dicarbonitriles.
Laboratorio De Radicales Libres Y QuíMica Computacional (Iqog, Csic)
Synthesis of physostigmine analogues and evaluation of their anticholinesterase activities.
Zhejiang University
Design, synthesis and evaluation of flavonoid derivatives as potent AChE inhibitors.
Zhejiang University
Synthesis and anti-acetylcholinesterase activity of 1-benzyl-4-[(5,6-dimethoxy-1-indanon-2-yl)methyl]piperidine hydrochloride (E2020) and related compounds
TBA
The synthesis and in vitro acetylcholinesterase and butyrylcholinesterase inhibitory activity of tacrine (Cognex®) derivaties
TBA
Site-activated multifunctional chelator with acetylcholinesterase and neuroprotective-neurorestorative moieties for Alzheimer's therapy.
Institute of Science
NO-donating tacrine hybrid compounds improve scopolamine-induced cognition impairment and show less hepatotoxicity.
Friedrich-Schiller-University Jena
2-Phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors: a study on the importance of modifications at the side chain on the activity.
Zhejiang University
Design, synthesis and evaluation of galanthamine derivatives as acetylcholinesterase inhibitors.
Zhejiang University
Design, synthesis and AChE inhibitory activity of indanone and aurone derivatives.
Zhejiang University
Design, synthesis and pharmacological evaluation of hybrid molecules out of quinazolinimines and lipoic acid lead to highly potent and selective butyrylcholinesterase inhibitors with antioxidant properties.
Friedrich-Schiller-UniversitäT Jena
Chemiluminescent high-throughput microassay applied to imidazo[2,1-b]thiazole derivatives as potential acetylcholinesterase and butyrylcholinesterase inhibitors.
Università
Methyl 2-(2-(4-formylphenoxy)acetamido)-2-substituted acetate derivatives: a new class of acetylcholinesterase inhibitors.
Sun Yat-Sen University
Review of bioactivity and structure-activity relationship on baicalein (5,6,7-trihydroxyflavone) and wogonin (5,7-dihydroxy-8-methoxyflavone) derivatives: Structural modifications inspired from flavonoids in Scutellaria baicalensis.
Shaanxi University of Chinese Medicine
Study on dual-site inhibitors of acetylcholinesterase: Highly potent derivatives of bis- and bifunctional huperzine B.
Chinese Academy of Sciences
Complexes of alkylene-linked tacrine dimers with Torpedo californica acetylcholinesterase: Binding of Bis5-tacrine produces a dramatic rearrangement in the active-site gorge.
Institute of Science
Homobivalent quinazolinimines as novel nanomolar inhibitors of cholinesterases with dirigible selectivity toward butyrylcholinesterase.
Friedrich-Schiller-UniversitäT Jena
Recent advance on carbamate-based cholinesterase inhibitors as potential multifunctional agents against Alzheimer's disease.
Lanzhou University
Development of naringenin-O-carbamate derivatives as multi-target-directed liagnds for the treatment of Alzheimer's disease.
Nanyang Normal University
Isolation and cholinesterase-inhibition studies of sterols from Haloxylon recurvum.
University of Karachi
Alzheimer's disease: Updated multi-targets therapeutics are in clinical and in progress.
Guizhou Medical University
Synthesis and acetylcholinesterase inhibition of derivatives of huperzine B.
Chinese Academy of Sciences
A tacrine-tetrahydroquinoline heterodimer potently inhibits acetylcholinesterase activity and enhances neurotransmission in mice.
The Hong Kong University of Science and Technology
Cage amines as the stopper inhibitors of cholinesterases.
National Chung-Hsing University
Design, synthesis and evaluation of novel dimethylamino chalcone-O-alkylamines derivatives as potential multifunctional agents against Alzheimer's disease.
Nanyang Normal University
Kinetics-Driven Drug Design Strategy for Next-Generation Acetylcholinesterase Inhibitors to Clinical Candidate.
Chinese Academy of Sciences
Design, synthesis, and pharmacological profile of novel fused pyrazolo[4,3-d]pyridine and pyrazolo[3,4-b][1,8]naphthyridine isosteres: a new class of potent and selective acetylcholinesterase inhibitors.
Universidade Federal Do Rio De Janeiro
Novel 3-benzylidene/benzylphthalide Mannich base derivatives as potential multifunctional agents for the treatment of Alzheimer's disease.
Guizhou Medical University
Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease.
Nanyang Normal University
Design, synthesis and evaluation of phthalide alkyl tertiary amine derivatives as promising acetylcholinesterase inhibitors with high potency and selectivity against Alzheimer's disease.
Guizhou Medical University
Discovery of 4'-OH-flurbiprofen Mannich base derivatives as potential Alzheimer's disease treatment with multiple inhibitory activities.
Sichuan University
Discovery of novel 2,5-dihydroxyterephthalamide derivatives as multifunctional agents for the treatment of Alzheimer's disease.
Sichuan University
Multi-target design strategies for the improved treatment of Alzheimer's disease.
China Pharmaceutical University
Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018).
Csir-Central Drug Research Institute
Multi-target-directed-ligands acting as enzyme inhibitors and receptor ligands.
Julius Maximilian University of W£Rzburg
Synthesis and comparison of the biological activity of monocyclic phosphonate, difluorophosphonate and phosphate analogs of the natural AChE inhibitor cyclophostin.
University of Missouri-St. Louis
Discovery of indanone derivatives as multi-target-directed ligands against Alzheimer's disease.
Sun Yat-Sen University
Novel benzisoxazole derivatives as potent and selective inhibitors of acetylcholinesterase.
Pfizer
Discovery of novel 2,6-disubstituted pyridazinone derivatives as acetylcholinesterase inhibitors.
Chinese Academy of Sciences
Homo- and hetero-dimers of inactive organophosphorous group binding at dual sites of AChE.
Chinese Academy of Agricultural Sciences
Development and biological activity of a new antagonist of the pheromone of the codling moth Cydia pomonella.
University of Lleida
Discovery of novel propargylamine-modified 4-aminoalkyl imidazole substituted pyrimidinylthiourea derivatives as multifunctional agents for the treatment of Alzheimer's disease.
East China University of Science and Technology
Design, synthesis and evaluation of vilazodone-tacrine hybrids as multitarget-directed ligands against depression with cognitive impairment.
East China University of Science and Technology
Design, synthesis and biological evaluation of phthalimide-alkylamine derivatives as balanced multifunctional cholinesterase and monoamine oxidase-B inhibitors for the treatment of Alzheimer's disease.
Nanyang Normal University
Synthesis and structure-activity relationships of acetylcholinesterase inhibitors: 1-benzyl-4-(2-phthalimidoethyl)piperidine and related derivatives.
Eisai
Compounds for use in methods for treating diseases or conditions mediated by protein disulfide isomerase
Beth Israel Deaconess Medical Center
Isoxazole compounds as inhibitors of heat shock proteins
The Institute of Cancer Research
The mobility of a conserved tyrosine residue controls isoform-dependent enzyme-inhibitor interactions in nitric oxide synthases.
University of California Irvine
Synthesis and evaluation of c-Src kinase inhibitory activity of pyridin-2(1H)-one derivatives.
University of Delhi
Trypsin-like serine protease inhibitors, and their preparation and use
The Medicines Company (Leipzig)
Tetrahydro-pyrazolo[1,5-a]pyrido-pyrimidines as antagonists of serotonin 5-HT6 receptors, methods for the production and use thereof
TBA
Substituted 4-(indazolyl)-1,4-dihydropyridines and methods of use thereof
Bayer Intellectual Property
Novel benzimidazole inhibitors bind to a unique site in the kinesin spindle protein motor domain.
Merck Research Laboratories
Genetic and pharmacological inhibition of PDK1 in cancer cells: characterization of a selective allosteric kinase inhibitor.
Merck Research Laboratories
Cisplatin inhibits protein splicing, suggesting inteins as therapeutic targets in mycobacteria.
University of Science and Technology of China
Discovery and SAR of 1,3,4-thiadiazole derivatives as potent Abl tyrosine kinase inhibitors and cytodifferentiating agents.
Universit&Aagrov
Computational study of antagonist/alpha1A adrenoceptor complexes--observations of conformational variations on the formation of ligand/receptor complexes.
University of Dublin
S33084, a novel, potent, selective, and competitive antagonist at dopamine D(3)-receptors: I. Receptorial, electrophysiological and neurochemical profile compared with GR218,231 and L741,626.
Centre De Recherches De Croissy
Characterization of human A(2B) adenosine receptors: radioligand binding, western blotting, and coupling to G(q) in human embryonic kidney 293 cells and HMC-1 mast cells.
University of Virginia
Functional effects of the muscarinic receptor agonist, xanomeline, at 5-HT1 and 5-HT2 receptors.
Smithkline Beecham Pharmaceuticals
Molecular pharmacology of homologues of ibotenic acid at cloned metabotropic glutamic acid receptors.
The Royal Danish School of Pharmacy
Pharmacology of [3H]prostaglandin E1/[3H]prostaglandin E2 and [3H]prostaglandin F2alpha binding to EP3 and FP prostaglandin receptor binding sites in bovine corpus luteum: characterization and correlation with functional data.
Alcon Laboratories
Nonpeptide endothelin receptor antagonists. XI. Pharmacological characterization of SB 234551, a high-affinity and selective nonpeptide ETA receptor antagonist.
Smithkline Beecham Pharmaceuticals
[3H]BIMU-1, a 5-hydroxytryptamine3 receptor ligand in NG-108 cells, selectively labels sigma-2 binding sites in guinea pig hippocampus.
Syntex Discovery Research
Cloning and expression of a human somatostatin-14-selective receptor variant (somatostatin receptor 4) located on chromosome 20.
University of Toronto
PET examination of [11C]NNC 687 and [11C]NNC 756 as new radioligands for the D1-dopamine receptor.
Karolinska Institutet
Cyclodextrin Inclusion Complexes: Studies of the Variation in the Size of Alicyclic Guests
University of Mississippi
7-Chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoyl-amino)benzoyl ]-2,3,4,5-tetrahydro-1H-1-benzazepine (OPC-41061): a potent, orally active nonpeptide arginine vasopressin V2 receptor antagonist.
Otsuka Pharmaceutical
Discovery, SAR, and pharmacokinetics of a novel 3-hydroxyquinolin-2(1H)-one series of potent D-amino acid oxidase (DAAO) inhibitors.
Pfizer
Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A.
Sphinx Laboratories
Synthesis and evaluation of 2-pyridinone derivatives as specific HIV-1 reverse transcriptase inhibitors. 3. Pyridyl and phenyl analogs of 3-aminopyridin-2(1H)-one.
Merck Research Laboratories
Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
Sapienza University of Rome
Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors.
Upjohn