Author/Editor		Knez, Damijan; Sosič, Izidor; Mitrović, Ana; Pišlar, Anja; Kos, Janko; Gobec, Stanislav
Title		8-hydroxyquinoline-based anti-Alzheimer multimodal agents
Type		članek
Vol. and No.		, št. Vol. 151
Publication year		2020
Volume		str. 1111-1120
ISSN		0026-9247 - Monatshefte für Chemie : Chemical Monthly
Language		eng
Abstract		The concept of multitarget-directed ligands (MTDLs) has attracted considerable interest in the development of agents against Alzheimer's disease. Cathepsin B, a cysteine protease, and butyrylcholinesterase, a serine hydrolase, play important function in the development and progression of Alzheimer's disease. We present herein the evaluation of 8-hydroxyquinoline-based analogues with activities against butyrylcholinesterase and %-secretase activity of cathepsin B. Furthermore, inhibition of amyloid [beta] aggregation, chelation of copper and zinc ions coupled with antioxidative properties and safe cytotoxicity profile of (1R,2S)-N-ethyl-2-[[(8-hydroxy-5-nitroquinolin-7-yl)methyl]amino]cyclohexane-1-carboxamide suggest that this derivative is a good starting point for optimization towards an effective multifunctional ligand.
Descriptors		Alzheimerjeva bolezen
Keywords		katepsin B holinesteraze ligandi Alzheimer's disease cathepsin B cholinesterases enzymes ligands aggregation