New tacrine-huperzine A hybrids (huprines): Highly potent tight-binding acetylcholinesterase inhibitors of interest for the treatment of Alzheimer's Disease

Journal of Medicinal Chemistry

Volumn 43, Issue 24, 2000, Pages 4657-4666

  Camps, P ^a   El Achab, R ^a   Morral, J ^a   Munoz Torrero, D ^a   Badia, A ^b   Eladi Banos, J ^b   Vivas, N M ^b   Barril, X ^a   Orozco, M ^a   Javier Luque, F ^b  

^a UNIVERSITY OF BARCELONA   (Spain)

^b UNIVERSITAT AUTÒNOMA DE BARCELONA   (Spain)

Author keywords

[No Author keywords available]

Indexed keywords

CHOLINESTERASE INHIBITOR; HUPERZINE A; HUPRINE; TACRINE DERIVATIVE; UNCLASSIFIED DRUG;

ALZHEIMER DISEASE; ARTICLE; DRUG EFFICACY; DRUG MECHANISM; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; HYBRID; NONHUMAN;

ACETYLCHOLINESTERASE; ALZHEIMER DISEASE; ANIMALS; BICYCLO COMPOUNDS; BUTYRYLCHOLINESTERASE; CATTLE; CHOLINESTERASE INHIBITORS; HUMANS; MALE; MICE; MODELS, MOLECULAR; NEUROMUSCULAR JUNCTION; NEUROMUSCULAR NONDEPOLARIZING AGENTS; NEUROPROTECTIVE AGENTS; QUINOLINES; RATS; RATS, SPRAGUE-DAWLEY; SESQUITERPENES; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; TACRINE; TUBOCURARINE;

EID: 0034736034     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm000980y     Document Type: Article

References (46)

1. Regional differences in the incidence of dementia in Europe-EURODEM collaborative analysis
2. The medicinal chemistry of Alzheimer and Alzheimer-like diseases with emphasis on the cholinergic hypothesis
3. Tacrine
4. Galanthamine in Alzheimer's disease. A new alternative to tacrine?
5. Synthesis and structure-activity relationships of acetylcholinesterase inhibitors: 1-Benzyl-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl]-piperidine Hydrochloride and related compounds
6. SDZ-ENA-713 cognition enhancer acetylcholinesterase inhibitor
7. Identification of a more potent analogue of the naturally ocurring alkaloid huperzine A. Predictive molecular modeling of its interaction with AChE
8. Chemistry, pharmacology, and clinical efficacy of the chinese nootropic agent huperzine A
9. Huperzine A, a potential therapeutic agent for treatment of Alzheimer's disease
10. Highly potent, selective, and low cost bis-tetrahydroaminacrine inhibitors of acetylcholinesterase
11. Evaluation of short-tether Bis-THA AChE inhibitors. A further test of the dual binding site hypothesis
12. Heterodimeric tacrine-based acetylcholinesterase inhibitors: Investigating ligand-peripheral site interactions
13. Potent, easily synthesized huperzine a-tacrine hybrid acetylcholinesterase inhibitors
14. Dimerization of an inactive fragment of huperzine A produces a drug with twice the potency of the natural product
15. Potent acetylcholinesterase inhibitors: Design, synthesis, and structure-activity relationships of bis-interacting ligands in the galanthamine series
16. Synthesis and acetyleholinesterase inhibitory activity of huperzine A-E2020 combined compound
17. 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
18. Predicting relative free energies of tacrine-huperzine A hybrids as inhibitors of acetylcholinesterase
19. Enantioselective synthesis of tacrine-huperzine A hybrids. Preparative chiral MPLC separation of their racemic mixtures and absolute configuration assignments by X-ray diffraction analysis
20. Huprine X is a novel high-affinity inhibitor of acetylcholinesterase that is of interest for treatment of Alzheimer's Disease
21. Easy synthesis of 7-Alkylbicyclo[3.3.1]non-6-en-3-ones by silica gel-promoted fragmentation of 3-Alkyl-2-oxaadamant-1-yl mesylates
22. Cyclization of ylidene-halodinitriles and ylidenecyanoacetates obtained from mesityl oxide and pulegone
23. Neuroleptic piperazinyl derivatives of 10H-Thieno[3,2-c][1]benzazepines and 4H-Thieno[2,3-c][1]-benzazepines
24. On the synthesis of 2-Amino-4,6-difluorobenzonitrile: Highly selective formation of 5-Fluoro-3-nitro-1,2-benzoquinone 2-Diazide in the attempted sandmeyer cyanation of 2,4-Difluoro-6-nitrobenzenediazonium cation
25. Synthesis of 2-Chloro-4-acetylaminobenzonitrile isomeres. Structurally related compounds with biological activities
26. Some acyl derivatives of bromoanthranilic nitrile, and the 7-Methyl-4-ketodihydroquinazolines prepared therefrom
27. Synthesis and Evaluation of Tacrine-Related Compounds for the Treatment of Alzheimer's Disease
28. Synthesis and evaluation of tacrine-huperzine A hybrids as acetylcholinesterase inhibitors of potential interest for the treatment of Alzheimer's Disease
29. A new and rapid colorimetric determination of acetylcholinesterase activity
30. Is there a Rationale for the Use of Acetylcholinesterase Inhibitors in the Therapy of Alzheimer's Disease?
31. Facilitatory action of adrenergic drugs on muscle twich evoked by nerve stimulation in the curarized rat phrenic-hemidiaphragm
32. Antagonism of non-depolarizing neuromuscular blockade by aminopyridines in cats
33. Binding of tacrine and 6-Chlorotacrine by acetylcholinesterase
34. Comparison of sample potential functions for simulating liquid water
35. Determining the contributions of constraints in free energy calculations: Development, characterization, and recommendations
36. Second generation force field for the simulation of proteins, nucleic acids, and organic molecules
37. A well-behaved electrostatic potential based method using charge restraints for deriving atomic charges
38. Numerical integration of the cartesian equations of motion of a system with constraints: Molecular dynamics of n-alkanes