Biginelli Reaction Synthesis of Novel Multitarget-Directed Ligands with Ca2+ Channel Blocking Ability, Cholinesterase Inhibition, Antioxidant Capacity, and Nrf2 Activation

Autor:	Rim Malek, Alexey Simakov, Audrey Davis, Maciej Maj, Paul J. Bernard, Artur Wnorowski, Helene Martin, José Marco-Contelles, Fakher Chabchoub, Patrick Dallemagne, Christophe Rochais, Krzysztof Jozwiak, Lhassane Ismaili
Jazyk:	angličtina
Rok vydání:	2022
Předmět:	Biginelli reaction multitarget-directed ligands calcium channel antagonism Nrf2 Organic chemistry QD241-441
Zdroj:	Molecules, Vol 28, Iss 1, p 71 (2022)
Druh dokumentu:	article
ISSN:	1420-3049
DOI:	10.3390/molecules28010071
Popis:	Novel multitarget-directed ligands BIGI 4a-d and BIGI 5a-d were designed and synthesized with a simple and cost-efficient procedure via a one-pot three-component Biginelli reaction targeting acetyl-/butyrylcholinesterases inhibition, calcium channel antagonism, and antioxidant ability. Among these multitarget-directed ligands, BIGI 4b, BIGI 4d, and BIGI 5b were identified as promising new hit compounds showing in vitro balanced activities toward the recognized AD targets. In addition, these compounds showed suitable physicochemical properties and a good druglikeness score predicted by Data Warrior software.
Databáze:	Directory of Open Access Journals
Externí odkaz:	https://doaj.org/article/c1008cfa0311472f9605360beca986c5 Zobrazit plný text záznamu View record in DOAJ Plný text ve formátu PDF Plný text ve formátu HTML
Nepřihlášeným uživatelům se plný text nezobrazuje	K zobrazení výsledku je třeba se přihlásit.