Multidirectional in vitro and in cellulo studies as a tool for identification of multi-target-directed ligands aiming at symptoms and causes of Alzheimer’s disease

Autor: Natalia Szałaj, Justyna Godyń, Jakub Jończyk, Anna Pasieka, Dawid Panek, Tomasz Wichur, Krzysztof Więckowski, Paula Zaręba, Marek Bajda, Anja Pislar, Barbara Malawska, Raimon Sabate, Anna Więckowska

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 35, Iss 1, Pp 1944-1952 (2020)

Effective therapy of Alzheimer’s disease (AD) requires treatment with a combination of drugs that modulate various pathomechanisms contributing to the disease. In our research, we have focused on the development of multi-target-directed ligands –

Externí odkaz: https://doaj.org/article/8664353705ab4c3dbfa4416d81bfa9d5

Synthesis, Molecular Modelling and Biological Evaluation of Novel Heterodimeric, Multiple Ligands Targeting Cholinesterases and Amyloid Beta

Autor: Michalina Hebda, Marek Bajda, Anna Więckowska, Natalia Szałaj, Anna Pasieka, Dawid Panek, Justyna Godyń, Tomasz Wichur, Damijan Knez, Stanislav Gobec, Barbara Malawska

Publikováno v: Molecules, Vol 21, Iss 4, p 410 (2016)

Cholinesterases and amyloid beta are one of the major biological targets in the search for a new and efficacious treatment of Alzheimer’s disease. The study describes synthesis and pharmacological evaluation of new compounds designed as dual bindin

Externí odkaz: https://doaj.org/article/6783527ad45f4c018b3bc70940f4a966

Dual Inhibitors of Amyloid-β and Tau Aggregation with Amyloid-β Disaggregating Properties: Extended In Cellulo, In Silico, and Kinetic Studies of Multifunctional Anti-Alzheimer’s Agents

Autor: Dawid Panek, Alba Espargaró, Marek Bajda, Anna Pasieka, Barbara Malawska, Anna Więckowska, Raimon Sabaté, Natalia Szałaj

Publikováno v: ACS Chemical Neuroscience

In Alzheimer’s disease, neurons slowly degenerate due to the accumulation of misfolded amyloid β and tau proteins. In our research, we performed extended studies directed at amyloid β and tau aggregation inhibition using in cellulo (Escherichia c

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::39ba40071bed94f96862fdb551c1c2b4
https://doi.org/10.1021/acschemneuro.1c00235

Design, synthesis, and biological evaluation of 2-(benzylamino-2-hydroxyalkyl)isoindoline-1,3-diones derivatives as potential disease-modifying multifunctional anti-Alzheimer agents

Autor: Marek Bajda, Dawid Panek, Anna Pasieka, Justyna Godyń, Barbara Malawska, Damijan Knez, Jakub Jończyk, Anna Więckowska, Stanislav Gobec

Publikováno v: Molecules, vol. 23, no. 2, 347, 2018.
Molecules : A Journal of Synthetic Chemistry and Natural Product Chemistry
Molecules; Volume 23; Issue 2; Pages: 347
Molecules, Vol 23, Iss 2, p 347 (2018)

The complex nature of Alzheimer's disease calls for multidirectional treatment. Consequently, the search for multi-target-directed ligands may lead to potential drug candidates. The aim of the present study is to seek multifunctional compounds with e

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::adac0a0f1687fb51eab76153ea0d9ddd
https://repozitorij.uni-lj.si/Dokument.php?id=149289&dn=

New Dual Small Molecules for Alzheimer’s Disease Therapy Combining Histamine H3 Receptor (H3R) Antagonism and Calcium Channels Blockade with Additional Cholinesterase Inhibition

Autor: Javier Egea, Daniel Diez-Iriepa, Barbara Mordyl, Alejandra Palomino-Antolín, Rim Malek, Lhassane Ismaili, Tereza Kobrlova, Justyna Godyń, Ondrej Soukup, José Marco-Contelles, Agata Siwek, Fakher Chabchoub, Ignacio Moraleda, Cristóbal de los Ríos, Dawid Panek, Céline Demougeot, Perle Totoson, Katarzyna Kieć-Kononowicz, Isabel Iriepa, Monika Głuch-Lutwin, Barbara Malawska, Raquel L Arribas

Publikováno v: Journal of Medicinal Chemistry. 62:11416-11422

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 activi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::30367824b94baa33e4e87aec58b11b2e
https://doi.org/10.1021/acs.jmedchem.9b00937