Discovery of 1-(phenylsulfonyl)-1H-indole-based multifunctional ligands targeting cholinesterases and 5-HT
| Autor: | Tomasz, Wichur, Anna, Pasieka, Justyna, Godyń, Dawid, Panek, Izabella, Góral, Gniewomir, Latacz, Ewelina, Honkisz-Orzechowska, Adam, Bucki, Agata, Siwek, Monika, Głuch-Lutwin, Damijan, Knez, Xavier, Brazzolotto, Stanislav, Gobec, Marcin, Kołaczkowski, Raimon, Sabate, Barbara, Malawska, Anna, Więckowska |
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| Rok vydání: | 2021 |
| Předmět: |
Amyloid beta-Peptides
Indoles Dose-Response Relationship Drug Molecular Structure tau Proteins Hep G2 Cells Ligands Molecular Docking Simulation Mice Protein Aggregates Structure-Activity Relationship Butyrylcholinesterase Receptors Serotonin Drug Discovery Electrophorus Acetylcholinesterase Microsomes Liver Animals Humans Cholinesterase Inhibitors Horses Cell Proliferation |
| Zdroj: | European journal of medicinal chemistry. 225 |
| ISSN: | 1768-3254 |
| Popis: | Multifunctional ligands as an essential variant of polypharmacology are promising candidates for the treatment of multi-factorial diseases like Alzheimer's disease. Based on clinical evidence and following the paradigm of multifunctional ligands we have rationally designed and synthesized a series of compounds targeting processes involved in the development of the disease. The biological evaluation led to the discovery of two compounds with favorable pharmacological characteristics and ADMET profile. Compounds 17 and 35 are 5-HT |
| Databáze: | OpenAIRE |
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