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Title:

Tacrine-Trolox Hybrids: A Novel Class of Centrally Active, Nonhepatotoxic Multi-Target-Directed Ligands Exerting Anticholinesterase and Antioxidant Activities with Low In Vivo Toxicity.

Document type:
Journal Article; Research Support, Non-U.S. Gov't
Author(s):
Nepovimova, Eugenie; Korabecny, Jan; Dolezal, Rafael; Babkova, Katerina; Ondrejicek, Ales; Jun, Daniel; Sepsova, Vendula; Horova, Anna; Hrabinova, Martina; Soukup, Ondrej; Bukum, Neslihan; Jost, Petr; Muckova, Lubica; Kassa, Jiri; Malinak, David; Andrs, Martin; Kuca, Kamil
Abstract:
Coupling of two distinct pharmacophores, tacrine and trolox, endowed with different biological properties, afforded 21 hybrid compounds as novel multifunctional candidates against Alzheimer's disease. Several of them showed improved inhibitory properties toward acetylcholinesterase (AChE) in relation to tacrine. These hybrids also scavenged free radicals. Molecular modeling studies in tandem with kinetic analysis exhibited that these hybrids target both catalytic active site as well as periphera...     »
Journal title abbreviation:
J Med Chem
Year:
2015
Journal volume:
58
Journal issue:
22
Pages contribution:
8985-9003
Language:
eng
Fulltext / DOI:
doi:10.1021/acs.jmedchem.5b01325
Pubmed ID:
http://view.ncbi.nlm.nih.gov/pubmed/26503905
Print-ISSN:
0022-2623
TUM Institution:
III. Medizinische Klinik und Poliklinik (Hämatologie / Onkologie)
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