| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 7754569 | Journal of Inorganic Biochemistry | 2016 | 44 Pages |
Abstract
Tacrine-(hydroxybenzoyl-pyridone) hybrids were designed, synthesized and evaluated as potential multitarget anti-Alzheimer's disease drugs. They are dual-binding site acetylcholinesterase inhibitors, with sub-micromolar activity as the parent tacrine, while the hydroxybenzoyl-pyridone moiety assures good radical scavenging capacity and moderate/good chelating power towards redox-active and/or amyloid-β-binding metal ions (Fe, Cu, Zn).299
Keywords
DCMHSQCDTNBTFADFPTACMTDLsCASTLCSDDAβBuChEESI-MSbutyrylcholinesteraseHEPESAnti-AChE activityDPPHDeferiproneHBPChEIs2,2-diphenyl-1-picrylhydrazyl4-(2-Hydroxyethyl)piperazine-1-ethanesulfonic acid5,5′-dithiobis-(2-nitrobenzoic acid)DFTDNAROSUV–Visamyloid-βAChAChEAcetylthiocholine iodideAcetylcholineAcetylcholinesterasedeoxyribonucleic acidTrifluoracetic acidUltraviolet–Visible SpectrophotometryAlzheimer's diseaseTacrineRoom temperaturePeripheral anionic sitecatalytic anionic siteMetal chelationHeteronuclear single quantum coherence spectroscopyElectrospray ionization-mass spectrometrycorrelation spectroscopyAnti-oxidant activityMulti-target-directed ligandscholinesterase inhibitorsDensity functional theoryPASHupAHuperzine ACOSYthin layer chromatographyReactive oxygen species
Related Topics
Physical Sciences and Engineering
Chemistry
Inorganic Chemistry
Authors
Karam Chand, Hesham M. Alsoghier, SÃlvia Chaves, M. Amélia Santos,