201 articles for thisTarget
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New azepino[4,3-b]indole derivatives as nanomolar selective inhibitors of human butyrylcholinesterase showing protective effects against NMDA-induced neurotoxicity.
University Of Bari&Quot;A. Moro&Quot
Novel multi-target-directed ligands for Alzheimer's disease: Combining cholinesterase inhibitors and 5-HT
Jagiellonian University Collegium Medicum
N-Propargylpiperidines with naphthalene-2-carboxamide or naphthalene-2-sulfonamide moieties: Potential multifunctional anti-Alzheimer's agents.
University Of Ljubljana
Synthesis and application ofß-carbolines as novel multi-functional anti-Alzheimer's disease agents.
University Of Massachusetts Boston
Synthesis and structure-activity relationship study of tacrine-based pyrano[2,3-c]pyrazoles targeting AChE/BuChE and 15-LOX.
Tehran University Of Medical Sciences
Rational modification of donepezil as multifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease.
China Pharmaceutical University
Design, synthesis, biological evaluation, and molecular modeling studies of chalcone-rivastigmine hybrids as cholinesterase inhibitors.
South China University Of Technology
Synthesis, structure-activity relationship and molecular docking of 3-oxoaurones and 3-thioaurones as acetylcholinesterase and butyrylcholinesterase inhibitors.
University Of Gujrat
Donepezil-like multifunctional agents: Design, synthesis, molecular modeling and biological evaluation.
Okayama University
New cinnamic - N-benzylpiperidine and cinnamic - N,N-dibenzyl(N-methyl)amine hybrids as Alzheimer-directed multitarget drugs with antioxidant, cholinergic, neuroprotective and neurogenic properties.
Instituto De Qu£Mica M£Dica
Novel series of tacrine-tianeptine hybrids: Synthesis, cholinesterase inhibitory activity, S100B secretion and a molecular modeling approach.
Universidade Federal Do Rio Grande Do Sul
Novel potent pyridoxine-based inhibitors of AChE and BChE, structural analogs of pyridostigmine, with improved in vivo safety profile.
Kazan (Volga Region) Federal University
Fatty Acid Amide Hydrolase (FAAH), Acetylcholinesterase (AChE), and Butyrylcholinesterase (BuChE): Networked Targets for the Development of Carbamates as Potential Anti-Alzheimer's Disease Agents.
Alma Mater Studiorum-University Of Bologna
Cholinesterase inhibitory activity of isoquinoline alkaloids from three Cryptocarya species (Lauraceae).
University Of Malaya
Synthesis and evaluation of multi-target-directed ligands for the treatment of Alzheimer's disease based on the fusion of donepezil and melatonin.
China Pharmaceutical University
Discovery of Highly Selective and Nanomolar Carbamate-Based Butyrylcholinesterase Inhibitors by Rational Investigation into Their Inhibition Mode.
Universit£T W£Rzburg
Amyloid cascade in Alzheimer's disease: Recent advances in medicinal chemistry.
University Of Waterloo
Application of PEG-400 as a green biodegradable polymeric medium for the catalyst-free synthesis of spiro-dihydropyridines and their use as acetyl and butyrylcholinesterase inhibitors.
Persian Gulf University
Design, synthesis and biological evaluation of novel donepezil-coumarin hybrids as multi-target agents for the treatment of Alzheimer's disease.
China Pharmaceutical University
Novel Tacrine-Benzofuran Hybrids as Potent Multitarget-Directed Ligands for the Treatment of Alzheimer's Disease: Design, Synthesis, Biological Evaluation, and X-ray Crystallography.
China Pharmaceutical University
Tacrine-Trolox Hybrids: A Novel Class of Centrally Active, Nonhepatotoxic Multi-Target-Directed Ligands Exerting Anticholinesterase and Antioxidant Activities with Low In Vivo Toxicity.
University Hospital Hradec Kralove
New multifunctional melatonin-derived benzylpyridinium bromides with potent cholinergic, antioxidant, and neuroprotective properties as innovative drugs for Alzheimer's disease.
1St Affiliated Hospital Of Guangxi Medical University
Synthesis of novel triazoles and a tetrazole of escitalopram as cholinesterase inhibitors.
University Of The Punjab
Design, synthesis and pharmacological evaluation of chalcone derivatives as acetylcholinesterase inhibitors.
Hu'Nan University
Structure-based development of nitroxoline derivatives as potential multifunctional anti-Alzheimer agents.
University Of Ljubljana
Structure-Based Design and Optimization of Multitarget-Directed 2H-Chromen-2-one Derivatives as Potent Inhibitors of Monoamine Oxidase B and Cholinesterases.
Universit£
Isolation of cholinesterase andß-secretase 1 inhibiting compounds from Lycopodiella cernua.
Catholic University Of Daegu
Multi-target tacrine-coumarin hybrids: cholinesterase and monoamine oxidase B inhibition properties against Alzheimer's disease.
China Pharmaceutical University
Multifunctional tacrine-trolox hybrids for the treatment of Alzheimer's disease with cholinergic, antioxidant, neuroprotective and hepatoprotective properties.
China Pharmaceutical University
N-Methyl-N-((1-methyl-5-(3-(1-(2-methylbenzyl)piperidin-4-yl)propoxy)-1H-indol-2-yl)methyl)prop-2-yn-1-amine, a new cholinesterase and monoamine oxidase dual inhibitor.
Laboratorio De Quimica Medica (Iqog, Csic)
New septanoside and 20-hydroxyecdysone septanoside derivative from Atriplex portulacoides roots with preliminary biological activities.
University Of Monastir
Synthesis and biological evaluation of novel tacrine derivatives and tacrine-coumarin hybrids as cholinesterase inhibitors.
P. J. Safarik University
Syntheses of coumarin-tacrine hybrids as dual-site acetylcholinesterase inhibitors and their activity against butylcholinesterase, Aß aggregation, andß-secretase.
Central China Normal University
Tetrahydrobenzo[h][1,6]naphthyridine-6-chlorotacrine hybrids as a new family of anti-Alzheimer agents targetingß-amyloid, tau, and cholinesterase pathologies.
Universitat De Barcelona
Sulfonamides as multifunctional agents for Alzheimer's disease.
University Of Massachusetts Boston
Multitarget drug design strategy: quinone-tacrine hybrids designed to block amyloid-ß aggregation and to exert anticholinesterase and antioxidant effects.
Alma Mater Studiorum-University Of Bologna
Active compounds from a diverse library of triazolothiadiazole and triazolothiadiazine scaffolds: synthesis, crystal structure determination, cytotoxicity, cholinesterase inhibitory activity, and binding mode analysis.
Quaid-I-Azam University
Discovery, biological evaluation, and crystal structure of a novel nanomolar selective butyrylcholinesterase inhibitor.
University Of Ljubljana
Design, synthesis and biological evaluation of novel 6H-benzo[c]chromen-6-one, and 7,8,9,10-tetrahydro-benzo[c]chromen-6-one derivatives as potential cholinesterase inhibitors.
Eastern Mediterranean University
Shogaol-huprine hybrids: dual antioxidant and anticholinesterase agents withß-amyloid and tau anti-aggregating properties.
Universitat De Barcelona
Synthesis ofa,ß-unsaturated carbonyl based compounds as acetylcholinesterase and butyrylcholinesterase inhibitors: characterization, molecular modeling, QSAR studies and effect against amyloidß-induced cytotoxicity.
Universiti Kebangsaan Malaysia
Dual inhibition of thea-glucosidase and butyrylcholinesterase studied by molecular field topology analysis.
University Of Florida
Design, synthesis and biological evaluation of benzylisoquinoline derivatives as multifunctional agents against Alzheimer's disease.
China Pharmaceutical University
Synthesis and multitarget biological profiling of a novel family of rhein derivatives as disease-modifying anti-Alzheimer agents.
Universitat De Barcelona
Synthesis, crystal structure and biological evaluation of some novel 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazoles and 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazines.
Quaid-I-Azam University
Synthesis, cytotoxicity and molecular modelling studies of new phenylcinnamide derivatives as potent inhibitors of cholinesterases.
Quaid-I-Azam University
Multifunctional cholinesterase and amyloid Beta fibrillization modulators. Synthesis and biological investigation.
University Of Siena
Preparation, in vitro evaluation and molecular modelling of pyridinium-quinolinium/isoquinolinium non-symmetrical bisquaternary cholinesterase inhibitors.
Charles University In Prague
Synthesis, evaluation and molecular dynamics study of some new 4-aminopyridine semicarbazones as an antiamnesic and cognition enhancing agents.
Banaras Hindu University
Synthesis of tacrine-lophine hybrids via one-pot four component reaction and biological evaluation as acetyl- and butyrylcholinesterase inhibitors.
Universidade Federal Do Rio Grande Do Sul
Design, synthesis and biological evaluation of coumarin alkylamines as potent and selective dual binding site inhibitors of acetylcholinesterase.
Universit£
Structure-activity relationships of methoctramine-related polyamines as muscarinic antagonist: effect of replacing the inner polymethylene chain with cyclic moieties.
Universit£
Hexahydrochromeno[4,3-b]pyrrole derivatives as acetylcholinesterase inhibitors.
University Of Bologna
Synthesis, biological assessment, and molecular modeling of racemic 7-aryl-9,10,11,12-tetrahydro-7H-benzo[7,8]chromeno[2,3-b]quinolin-8-amines as potential drugs for the treatment of Alzheimer's disease.
Universit£
Exploration of natural compounds as sources of new bifunctional scaffolds targeting cholinesterases and beta amyloid aggregation: the case of chelerythrine.
Abo Akademi University
2-Arylbenzofuran-based molecules as multipotent Alzheimer's disease modifying agents.
University Of Bologna
Design, synthesis, and bioevaluation of benzamides: novel acetylcholinesterase inhibitors with multi-functions on butylcholinesterase, Aß aggregation, andß-secretase.
Central China Normal University
Radiolabeled cyclosaligenyl monophosphates of 5-iodo-2'-deoxyuridine, 5-iodo-3'-fluoro-2',3'-dideoxyuridine, and 3'-fluorothymidine for molecular radiotherapy of cancer: synthesis and biological evaluation.
University Of Nebraska Medical Center
Pyridonepezils, new dual AChE inhibitors as potential drugs for the treatment of Alzheimer's disease: synthesis, biological assessment, and molecular modeling.
Instituto De Qu£Mica Org£Nica General (Csic)
Synthesis, design and biological evaluation of novel highly potent tacrine congeners for the treatment of Alzheimer's disease.
P. J. Safarik 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)
New tacrine-4-oxo-4H-chromene hybrids as multifunctional agents for the treatment of Alzheimer's disease, with cholinergic, antioxidant, andß-amyloid-reducing properties.
Instituto De Qu£Mica M£Dica
Huprine-tacrine heterodimers as anti-amyloidogenic compounds of potential interest against Alzheimer's and prion diseases.
Universitat De Barcelona
Preparation, in vitro screening and molecular modelling of symmetrical 4-tert-butylpyridinium cholinesterase inhibitors--analogues of SAD-128.
University Of Defence
Long-acting anticholinesterases for myasthenia gravis: synthesis and activities of quaternary phenylcarbamates of neostigmine, pyridostigmine and physostigmine.
National Institute On Aging
Isosorbide-2-benzyl carbamate-5-salicylate, a peripheral anionic site binding subnanomolar selective butyrylcholinesterase inhibitor.
Trinity College
Structural aspects of flavonoids as inhibitors of human butyrylcholinesterase.
Institute For Medical Research And Occupational Health
Synthesis and structure-activity relationship of Huprine derivatives as human acetylcholinesterase inhibitors.
Cobra
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 4. Further investigation on the inner spacer.
University Of Bologna
New tacrine-dihydropyridine hybrids that inhibit acetylcholinesterase, calcium entry, and exhibit neuroprotection properties.
Laboratorio De Radicales Libres (Iqog, Csic)
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.
Universit£
Synthesis and biological evaluation of NO-donor-tacrine hybrids as hepatoprotective anti-Alzheimer drug candidates.
TBA
Multi-target-directed ligands to combat neurodegenerative diseases.
University Of Bologna
4-Aminopyridine derivatives with anticholinesterase and antiamnesic activity.
Sapienza University Of Rome
Novel class of quinone-bearing polyamines as multi-target-directed ligands to combat Alzheimer's disease.
University Of Bologna
Bis-cycloSal-d4T-monophosphates: drugs that deliver two molecules of bioactive nucleotides.
University Of Hamburg
Binding of 13-amidohuprines to acetylcholinesterase: exploring the ligand-induced conformational change of the gly117-gly118 peptide bond in the oxyanion hole.
Universitat De Barcelona
Novel anticholinesterases based on the molecular skeletons of furobenzofuran and methanobenzodioxepine.
National Institute On Aging
Further studies on the interaction of the 5-hydroxytryptamine3 (5-HT3) receptor with arylpiperazine ligands. development of a new 5-HT3 receptor ligand showing potent acetylcholinesterase inhibitory properties.
Universit£
Propidium-based polyamine ligands as potent inhibitors of acetylcholinesterase and acetylcholinesterase-induced amyloid-beta aggregation.
University Of Bologna
Interaction of cycloSal-pronucleotides with cholinesterases from different origins. A structure-activity relationship.
University Of Hamburg
Specific targeting of acetylcholinesterase and butyrylcholinesterase recognition sites. Rational design of novel, selective, and highly potent cholinesterase inhibitors.
Universit£
Synthesis, in vitro pharmacology, and molecular modeling of syn-huprines as acetylcholinesterase inhibitors.
Universitat De Barcelona
Design, synthesis, and structure-activity relationships of a series of 3-[2-(1-benzylpiperidin-4-yl)ethylamino]pyridazine derivatives as acetylcholinesterase inhibitors.
Universit£
New tacrine-huperzine A hybrids (huprines): highly potent tight-binding acetylcholinesterase inhibitors of interest for the treatment of Alzheimer's disease.
Universitat De Barcelona
Synthesis, in vitro pharmacology, and molecular modeling of very potent tacrine-huperzine A hybrids as acetylcholinesterase inhibitors of potential interest for the treatment of Alzheimer's disease.
Universitat De Barcelona
Acetylcholinesterase noncovalent inhibitors based on a polyamine backbone for potential use against Alzheimer's disease.
University Of Bologna
Design and synthesis of 1-heteroaryl-3-(1-benzyl-4-piperidinyl)propan-1-one derivatives as potent, selective acetylcholinesterase inhibitors.
Pfizer
Synthesis and cholinergic properties of bis[[(dimethylamino)methyl]furanyl] analogues of ranitidine.
University Of South Carolina
Binary antidotes for organophosphate poisoning: aprophen analogues that are both antimuscarinics and carbamates.
Institute Of Research
Amidine-oximes: reactivators for organophosphate exposure.
Human Biomolecular Research Institute
Nonquaternary reactivators for organophosphate-inhibited cholinesterases.
Human Biomolecular Research Institute
A review on coumarins as acetylcholinesterase inhibitors for Alzheimer's disease.
Punjabi University
Synthesis of monomeric derivatives to probe memoquin's bivalent interactions.
University Of Bologna
Synthesis, biological evaluation, and molecular modeling of donepezil and N-[(5-(benzyloxy)-1-methyl-1H-indol-2-yl)methyl]-N-methylprop-2-yn-1-amine hybrids as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's disease.
Universitat Aut£Noma De Barcelona
Synthesis and biological assessment of diversely substituted furo[2,3-b]quinolin-4-amine and pyrrolo[2,3-b]quinolin-4-amine derivatives, as novel tacrine analogues.
University Of Lisbon
Selective cholinesterase inhibition by lanostane triterpenes from fruiting bodies of Ganoderma lucidum.
Chungnam National University
Synthesis and in vitro evaluation of 7-methoxy-N-(pent-4-enyl)-1,2,3,4-tetrahydroacridin-9-amine-new tacrine derivate with cholinergic properties.
Charles University In Prague
Exploiting the lipoic acid structure in the search for novel multitarget ligands against Alzheimer's disease.
University Of Bologna
Multi-target strategy to address Alzheimer's disease: design, synthesis and biological evaluation of new tacrine-based dimers.
Institut F£R Molekulare Physiologie
Requirements for mammalian carboxylesterase inhibition by substituted ethane-1,2-diones.
St. Jude Children'S Research Hospital
Synthesis, biological activity and HPLC validation of 1,2,3,4-tetrahydroacridine derivatives as acetylcholinesterase inhibitors.
Medical University
New potent human acetylcholinesterase inhibitors in the tetracyclic triterpene series with inhibitory potency on amyloid β aggregation.
Cnrs
Synthesis and biological evaluation of novel gamma-carboline analogues of Dimebon as potent 5-HT6 receptor antagonists.
Chemical Diversity Research Institute
Novel carbamate cholinesterase inhibitors that release biologically active amines following enzyme inhibition.
Sention
Benzophenone-based derivatives: a novel series of potent and selective dual inhibitors of acetylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation.
University Of Bologna
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
Multitargeted drugs discovery: balancing anti-amyloid and anticholinesterase capacity in a single chemical entity.
Department Of Pharmaceutical Sciences-Alma Mater Studiorum-Bologna University
(+)-Arisugacin A--computational evidence of a dual binding site covalent inhibitor of acetylcholinesterase.
Alchemical Research
Preparation, in vitro screening and molecular modelling of symmetrical bis-quinolinium cholinesterase inhibitors--implications for early myasthenia gravis treatment.
Charles University
Preparation and in vitro screening of symmetrical bis-isoquinolinium cholinesterase inhibitors bearing various connecting linkage--implications for early Myasthenia gravis treatment.
University Of Defence
Structure-activity relationships of substituted 1-pyridyl-2-phenyl-1,2-ethanediones: potent, selective carboxylesterase inhibitors.
St. Jude Children'S Research Hospital
Synthesis, characterization, oxidative degradation, antibacterial activity and acetylcholinesterase/butyrylcholinesterase inhibitory effects of some new phosphorus(V) hydrazides.
Tarbiat Modares University
Synthesis and in vitro evaluation of N-alkyl-7-methoxytacrine hydrochlorides as potential cholinesterase inhibitors in Alzheimer disease.
Charles University
Novel tacrine-8-hydroxyquinoline hybrids as multifunctional agents for the treatment of Alzheimer's disease, with neuroprotective, cholinergic, antioxidant, and copper-complexing properties.
Instituto De Quimica Medica
Preparation and in vitro screening of symmetrical bispyridinium cholinesterase inhibitors bearing different connecting linkage-initial study for Myasthenia gravis implications.
Military Health Sciences
Neuroprotective and cholinergic properties of multifunctional glutamic acid derivatives for the treatment of Alzheimer's disease.
Instituto De Quimica Medica (Csic)
Differential binding of phenothiazine urea derivatives to wild-type human cholinesterases and butyrylcholinesterase mutants.
Dalhousie University
Targeting Alzheimer's disease: Novel indanone hybrids bearing a pharmacophoric fragment of AP2238.
University Of Bologna
Isosorbide-based cholinesterase inhibitors; replacement of 5-ester groups leading to increased stability.
Trinity College
Toward a rational design of multitarget-directed antioxidants: merging memoquin and lipoic acid molecular frameworks.
University Of Bologna
Synthesis of novel purine nucleosides towards a selective inhibition of human butyrylcholinesterase.
Faculdade De Ci£Ncias Da Universidade De Lisboa
Structure-activity relationships of memoquin: Influence of the chain chirality in the multi-target mechanism of action.
Alma Mater Studiorum-Bologna University
Antioxidant and anticholinesterase activity evaluation of ent-kaurane diterpenoids from Sideritis arguta.
Istanbul University
Synthesis and preliminary structure-activity relationships of 1-[(3-fluoro-4-pyridinyl)amino]-3-methyl-1H-indol-5-yl methyl carbamate (P10358), a novel acetylcholinesterase inhibitor
TBA
Isosorbide-2-carbamate esters: potent and selective butyrylcholinesterase inhibitors.
Trinity College
Tacrine based human cholinesterase inhibitors: synthesis of peptidic-tethered derivatives and their effect on potency and selectivity.
European Research Centre For Drug Discovery And Development (Natsyndrugs)
Synthesis and biological evaluation of (-)- and (+)-debromoflustramine B and its analogues as selective butyrylcholinesterase inhibitors.
Instituto PolitéCnico Nacional
Bioactive 5alpha-pregnane-type steroidal alkaloids from Sarcococca hookeriana.
Bielefeld University
Solid-phase synthesis and biological evaluation of a parallel library of 2,3-dihydro-1,5-benzothiazepines.
Quaid-I-Azam University
Inhibition of acetylcholinesterase, beta-amyloid aggregation, and NMDA receptors in Alzheimer's disease: a promising direction for the multi-target-directed ligands gold rush.
University Of Bologna
Carbamates with differential mechanism of inhibition toward acetylcholinesterase and butyrylcholinesterase.
Dalhousie University
Design, synthesis and evaluation of isaindigotone derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors.
Sun Yat-Sen University
Benzofuran-based hybrid compounds for the inhibition of cholinesterase activity, beta amyloid aggregation, and abeta neurotoxicity.
University Of Bologna
Design, synthesis, and evaluation of benzophenone derivatives as novel acetylcholinesterase inhibitors.
University Of Bologna
New triterpenoid alkaloid cholinesterase inhibitors from Buxus hyrcana.
University Of Karachi
Multi-target-directed drug design strategy: from a dual binding site acetylcholinesterase inhibitor to a trifunctional compound against Alzheimer's disease.
Bologna University
Synthesis and structure-activity relationship for a novel class of potent and selective carbamate-based inhibitors of hormone selective lipase with acute in vivo antilipolytic effects.
Novo Nordisk
Synthesis, in vitro assay, and molecular modeling of new piperidine derivatives having dual inhibitory potency against acetylcholinesterase and Abeta1-42 aggregation for Alzheimer's disease therapeutics.
Woosuk University
Selective reversible inhibition of human butyrylcholinesterase by aryl amide derivatives of phenothiazine.
Dalhousie University
Extensive SAR and computational studies of 3-{4-[(benzylmethylamino)methyl]phenyl}-6,7-dimethoxy-2H-2-chromenone (AP2238) derivatives.
University Of Bologna
Analysis of the inhibition of mammalian carboxylesterases by novel fluorobenzoins and fluorobenzils.
St. Jude Children'S Research Hospital
Novel multipotent tacrine-dihydropyridine hybrids with improved acetylcholinesterase inhibitory and neuroprotective activities as potential drugs for the treatment of Alzheimer's disease.
Laboratorio De Radicales Libres (Iqog, Csic)
Cholinesterase inhibitors: SAR and enzyme inhibitory activity of 3-[omega-(benzylmethylamino)alkoxy]xanthen-9-ones.
University Of Bologna
6-Hydroxy- and 6-methoxy-beta-carbolines as acetyl- and butyrylcholinesterase inhibitors.
Friedrich-Schiller-UniversitäT Jena
cycloSal-PMEA and cycloAmb-PMEA: potentially new phosphonate prodrugs based on the cycloSal-pronucleotide approach.
University Of Hamburg
Isoterreulactone A, a novel meroterpenoid with anti-acetylcholinesterase activity produced by Aspergillus terreus.
Korea Research Institute Of Bioscience And Biotechnology
Synthesis and structure-activity relationship for a novel class of potent and selective carbamoyl-triazole based inhibitors of hormone sensitive lipase.
Novo Nordisk
Molecular docking studies of natural cholinesterase-inhibiting steroidal alkaloids from Sarcococca saligna.
University Of Innsbruck
Synthesis and structure-activity relationships of open D-Ring galanthamine analogues.
Cnrs
Synthesis of novel phenserine-based-selective inhibitors of butyrylcholinesterase for Alzheimer's disease.
National Institute On Aging Intramural Research Program
Synthesis of dihydroxanthone derivatives and evaluation of their inhibitory activity against acetylcholinesterase: unique structural analogs of tacrine based on the BCD-ring of arisugacin.
University Of Minnesota
Novel tacrine analogues for potential use against Alzheimer's disease: potent and selective acetylcholinesterase inhibitors and 5-HT uptake inhibitors.
University Of Strathclyde
Total syntheses and anticholinesterase activities of (3aS)-N(8)-norphysostigmine, (3aS)-N(8)-norphenserine, their antipodal isomers, and other N(8)-substituted analogues.
National Institute On Aging
5,7-dihydro-3-[2-[1-(phenylmethyl)-4-piperidinyl]ethyl]-6H- pyrrolo[3,2-f]-1,2-benzisoxazol-6-one: a potent and centrally-selective inhibitor of acetylcholinesterase with an improved margin of safety.
Pfizer
Alfred Burger award address. Bioactive alkaloids. 4. Results of recent investigations with colchicine and physostigmine.
Niddk
Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine.
University Of South Carolina
Investigating the Reaction Mechanism of F420-Dependent Glucose-6-phosphate Dehydrogenase from Mycobacterium tuberculosis: Kinetic Analysis of the Wild-Type and Mutant Enzymes.
The University Of Texas At Arlington
Rofecoxib [Vioxx, MK-0966; 4-(4'-methylsulfonylphenyl)-3-phenyl-2-(5H)-furanone]: a potent and orally active cyclooxygenase-2 inhibitor. Pharmacological and biochemical profiles.
Merck Frosst Centre For Therapeutic Research
Cloning, expression and pharmacological characterization of rabbit adenosine A1 and A3 receptors.
Pfizer
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.
University Of California San Francisco
Discovery and SAR of 2-(1-propylpiperidin-4-yl)-1H-benzimidazole-4-carboxamide: A potent inhibitor of poly(ADP-ribose) polymerase (PARP) for the treatment of cancer.
Abbott Laboratories
Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity.
Astex
Potent inhibitors of HCV-NS3 protease derived from boronic acids.
Schering-Plough Research Institute
Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV.
University Of Tampere
Structural Requirements for Eszopiclone and Zolpidem Binding to the gamma-Aminobutyric Acid Type-A (GABAA) Receptor Are Different.
University Of Wisconsin At Madison
Lead Optimization of 4-Acetylamino-2-(3,5-dimethylpyrazol-1-yl)-6-pyridylpyrimidines as A2A Adenosine Receptor Antagonists for the Treatment of Parkinson's Disease.
Neurocrine Bioscience
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), A New Histamine H4R Antagonist that Blocks Pain Responses against Carrageenan-Induced Hyperalgesia.
Abbott Laboratories
Indazole-Based Liver X Receptor (LXR) Modulators with Maintained Atherosclerotic Lesion Reduction Activity but Diminished Stimulation of Hepatic Triglyceride Synthesis
Wyeth Research
Identification of a new JNK inhibitor targeting the JNK-JIP interaction site.
Burnham Institute For Medical Research
Design and Synthesis of Orally Bioavailable Benzimidazoles as Raf Kinase Inhibitors.
Novartis
Structure-based approach to the development of potent and selective inhibitors of dihydrofolate reductase from cryptosporidium.
University Of Connecticut At Storrs
Biochemically based design of cyclooxygenase-2 (COX-2) inhibitors: facile conversion of nonsteroidal antiinflammatory drugs to potent and highly selective COX-2 inhibitors.
Vanderbilt University School Of Medicine
Structure-based design, synthesis, and structure-activity relationship studies of novel non-nucleoside adenosine deaminase inhibitors.
Fujisawa Pharmaceutical
A highly potent non-nucleoside adenosine deaminase inhibitor: efficient drug discovery by intentional lead hybridization.
Fujisawa Pharmaceutical
Planarity and constraint of the carbonyl groups in 1,2-diones are determinants for selective inhibition of human carboxylesterase 1.
St. Jude Research Hospital