Synthesis and biological assessment of KojoTacrines as new agents for Alzheimer's disease therapy
In view of the multifactorial nature of Alzheimer's disease (AD), multitarget small molecules (MTSM) represent the most potent and attractive therapeutic strategy to design new drugs for Alzheimer's disease therapy. The new MTSM KojoTacrines (KTs) were designed and synthesized by juxtaposi...
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Taylor & Francis Group,
2019-01-01T00:00:00Z.
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| 100 | 1 | 0 | |a Youssef Dgachi |e author |
| 700 | 1 | 0 | |a Hélène Martin |e author |
| 700 | 1 | 0 | |a Rim Malek |e author |
| 700 | 1 | 0 | |a Daniel Jun |e author |
| 700 | 1 | 0 | |a Jana Janockova |e author |
| 700 | 1 | 0 | |a Vendula Sepsova |e author |
| 700 | 1 | 0 | |a Ondrej Soukup |e author |
| 700 | 1 | 0 | |a Isabel Iriepa |e author |
| 700 | 1 | 0 | |a Ignacio Moraleda |e author |
| 700 | 1 | 0 | |a Emna Maalej |e author |
| 700 | 1 | 0 | |a M. Carmo Carreiras |e author |
| 700 | 1 | 0 | |a Bernard Refouvelet |e author |
| 700 | 1 | 0 | |a Fakher Chabchoub |e author |
| 700 | 1 | 0 | |a José Marco-Contelles |e author |
| 700 | 1 | 0 | |a Lhassane Ismaili |e author |
| 245 | 0 | 0 | |a Synthesis and biological assessment of KojoTacrines as new agents for Alzheimer's disease therapy |
| 260 | |b Taylor & Francis Group, |c 2019-01-01T00:00:00Z. | ||
| 500 | |a 1475-6366 | ||
| 500 | |a 1475-6374 | ||
| 500 | |a 10.1080/14756366.2018.1538136 | ||
| 520 | |a In view of the multifactorial nature of Alzheimer's disease (AD), multitarget small molecules (MTSM) represent the most potent and attractive therapeutic strategy to design new drugs for Alzheimer's disease therapy. The new MTSM KojoTacrines (KTs) were designed and synthesized by juxtaposition of selected pharmacophoric motifs from kojic acid and tacrine. Among them, 11-amino-2-(hydroxymethyl)-12-(3-methoxyphenyl)-7,9,10,12-tetrahydropyrano [2',3':5,6] pyrano[2,3-b]quinolin-4(8H)-one (KT2d) was identified as less-hepatotoxic than tacrine, at higher concentration, a moderate, but selective human acetylcholinesterase inhibitor (IC50 = 4.52 ± 0.24 µM), as well as an antioxidant agent (TE = 4.79) showing significant neuroprotection against Aβ1-40 at 3 µM and 10 µM concentrations. Consequently, KT2d is a potential new hit-ligand for AD therapy for further biological exploration. | ||
| 546 | |a EN | ||
| 690 | |a alzheimer disease | ||
| 690 | |a kojic acid | ||
| 690 | |a multitarget small molecules | ||
| 690 | |a tacrine | ||
| 690 | |a Therapeutics. Pharmacology | ||
| 690 | |a RM1-950 | ||
| 655 | 7 | |a article |2 local | |
| 786 | 0 | |n Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 34, Iss 1, Pp 163-170 (2019) | |
| 787 | 0 | |n http://dx.doi.org/10.1080/14756366.2018.1538136 | |
| 787 | 0 | |n https://doaj.org/toc/1475-6366 | |
| 787 | 0 | |n https://doaj.org/toc/1475-6374 | |
| 856 | 4 | 1 | |u https://doaj.org/article/e3c0e08c463645d08a8cc7dd58a4bda9 |z Connect to this object online. |