Tacrines as Therapeutic Agents for Alzheimer's Disease. IV. The Tacripyrines and Related Annulated Tacrines.
Hupertacrines
Multitarget small molecules
Tacripyrimedones
Tacripyrimidines
Tacripyrines
Journal
Chemical record (New York, N.Y.)
ISSN: 1528-0691
Titre abrégé: Chem Rec
Pays: United States
ID NLM: 101085550
Informations de publication
Date de publication:
May 2019
May 2019
Historique:
received:
10
09
2018
revised:
30
10
2018
accepted:
05
11
2018
pubmed:
30
11
2018
medline:
22
5
2019
entrez:
30
11
2018
Statut:
ppublish
Résumé
Notwithstanding the clinical use of tacrine was hampered by severe hepatotoxicity, tacrine still remains a reference scaffold in the search for new efficient drugs for Alzheimer's disease therapy. In this account we summarize the efforts toward the development and characterization of non-hepatotoxic tacripyrines and related tacrine analogues resulting from the substitution of the benzene ring by a 1,4-dihydropyridine, a 1,2,3,4-tetrahydropyrimidine or a pyridone nucleus. These efforts have successfully led to the identification of a number of promising hits endowed with interesting multifunctional profiles. These include the 4'-metoxytacripyrine (S)-ITH122, able to target cholinesterases (ChEs), beta-amyloid (Aβ) and Ca
Identifiants
pubmed: 30489012
doi: 10.1002/tcr.201800155
doi:
Substances chimiques
Amyloid beta-Peptides
0
Cholinesterase Inhibitors
0
Neuroprotective Agents
0
SCR1693
0
Tacrine
4VX7YNB537
Types de publication
Journal Article
Review
Langues
eng
Sous-ensembles de citation
IM
Pagination
927-937Informations de copyright
© 2019 The Chemical Society of Japan & Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.