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Design, synthesis and biological evaluation of 1-benzylamino-2-hydroxyalkyl derivatives as new potential disease-modifying multifunctional anti-Alzheimer's agents [Elektronski vir]Panek, Dawid ...The multitarget approach is a promising paradigm in drug discovery, potentially leading to new treatment options for complex disorders, such as Alzheimer's disease. Herein, we present the discovery ... of a unique series of 1-benzylamino-2-hydroxyalkyl derivatives combining inhibitory activity against butyrylcholinesterase, beta-secretase, beta-amyloid and tau protein aggregation, all related to mechanisms which underpin Alzheimer's disease. Notably, diphenylpropylamine derivative 10 showed balanced activity against both disease-modifying targets beta inhibition of beta-secretase (IC50 hBACE-1 = 41.60 microM), inhibition of amyloid beta aggregation (IC50 Abeta = 3.09 microM), inhibition of tau aggregation (55% at 10 microM), as well as against symptomatic targets: butyrylcholinesterase inhibition (IC50 hBuChE = 7.22 microM). It might represent an encouraging starting point for development of multifunctional disease-modifying anti-Alzheimer's agents.Source: ACS chemical neuroscience. - ISSN 1948-7193 (Vol. 9, issue 5, 2018, str. 1074-1094)Type of material - e-articlePublish date - 2018Language - englishCOBISS.SI-ID - 4465009
Author
Panek, Dawid |
Więckowska, Anna |
Jończyk, Jakub |
Godyń, Justyna |
Bajda, Marek |
Wichur, Tomasz |
Pasieka, Anna |
Knez, Damijan, farmacevt |
Pišlar, Anja |
Korabecny, Jan |
Soukup, Ondrej, Biomedicinist |
Sepsova, Vendula |
Sabaté, Raimon |
Kos, Janko, 1959- |
Gobec, Stanislav, 1970- |
Malawska, Barbara
Topics
Alzheimer's disease |
multifunctional agents |
butyrylcholinesterase inhibitors |
BACE-1 inhibitors |
Abeta aggregation |
tau aggregation |
molecular docking
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Panek, Dawid | ![]() |
Więckowska, Anna | ![]() |
Jończyk, Jakub | ![]() |
Godyń, Justyna | ![]() |
Bajda, Marek | ![]() |
Wichur, Tomasz | ![]() |
Pasieka, Anna | ![]() |
Knez, Damijan, farmacevt | 36438 |
Pišlar, Anja | 32035 |
Korabecny, Jan | ![]() |
Soukup, Ondrej, Biomedicinist | ![]() |
Sepsova, Vendula | ![]() |
Sabaté, Raimon | ![]() |
Kos, Janko, 1959- | 04648 |
Gobec, Stanislav, 1970- | 15284 |
Malawska, Barbara | ![]() |
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