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New Dual Small Molecules for Alzheimer's Disease Therapy Combining Histamine H3 Receptor (H3R) Antagonism and Calcium Channels Blockade with Additional Cholinesterase Inhibition
R. Malek, RL. Arribas, A. Palomino-Antolin, P. Totoson, C. Demougeot, T. Kobrlova, O. Soukup, I. Iriepa, I. Moraleda, D. Diez-Iriepa, J. Godyń, D. Panek, B. Malawska, M. Głuch-Lutwin, B. Mordyl, A. Siwek, F. Chabchoub, J. Marco-Contelles, K....
Journal of medicinal chemistry.
2019 ;
62 (24) :
11416-11422.
[pub] 20191205
Jazyk angličtina Země Spojené státy americké
Typ dokumentu časopisecké články, práce podpořená grantem
Perzistentní odkaz
https://www.medvik.cz/link/bmc20023309
- MeSH
- Alzheimerova nemoc farmakoterapie metabolismus MeSH
- blokátory kalciových kanálů chemie farmakologie MeSH
- cholinesterasové inhibitory chemie farmakologie MeSH
- knihovny malých molekul chemie farmakologie MeSH
- lidé MeSH
- myši MeSH
- nádorové buňky kultivované MeSH
- neuroblastom farmakoterapie metabolismus MeSH
- neuroprotektivní látky chemie farmakologie MeSH
- poruchy paměti farmakoterapie metabolismus MeSH
- receptory histaminu H3 chemie MeSH
- vazodilatancia chemie farmakologie MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- myši MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
New tritarget small molecules combining Ca2+ channels blockade, cholinesterase, and H3 receptor inhibition were obtained by multicomponent synthesis. Compound 3p has been identified as a very promising lead, showing good Ca2+ channels blockade activity (IC50 = 21 ± 1 μM), potent affinity against hH3R (Ki = 565 ± 62 nM), a moderate but selective hBuChE inhibition (IC50 = 7.83 ± 0.10 μM), strong antioxidant power (3.6 TE), and ability to restore cognitive impairment induced by lipopolysaccharide.
EA4267 PEPITE Université Bourgogne Franche Comté F 25030 Besançon France
Faculty of Pharmacy Jagiellonian University Medical College Medyczna 9 30 688 Kraków Poland
Laboratory of Medicinal Chemistry IQOG CSIC Juan de la Cierva 3 28006 Madrid Spain
Citace poskytuje Crossref.org
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