Synthesis and investigation of the cholinesterase inhibitory and antioxidant capacities of some novel N'‐(quinolin‐4‐ylmethylene)propanehydrazides against Alzheimer's disease

• Published in: Drug development research Vol. 85; no. 3; pp. e22183 - n/a
• Main Authors: Kilic, Burcu, Dogruer, Deniz S.
• Format: Journal Article
• Language: English
• Published: United States Wiley Subscription Services, Inc 01.05.2024
• Subjects: Acetylcholinesterase; Acetylcholinesterase - metabolism; Alzheimer Disease - drug therapy; Alzheimer's disease; antioxidant; Antioxidants; Antioxidants - pharmacology; Antioxidants - therapeutic use; Butyrylcholinesterase - metabolism; Cholinesterase; cholinesterase inhibition; Cholinesterase Inhibitors - pharmacology; Cholinesterase Inhibitors - therapeutic use; Drug development; Humans; Inhibitors; metal chelation; Molecular Docking Simulation; Neurodegenerative diseases; quinoline; Structure-Activity Relationship; antioxidant; cholinesterase inhibition; quinoline; metal chelation; Alzheimer's disease
• ISSN: 0272-4391; 1098-2299; 1098-2299
• DOI: 10.1002/ddr.22183

One of the worst long‐term health issues of the past few decades is Alzheimer's disease (AD). Unfortunately, there are currently insufficient choices for treating and caring for AD, which makes it a popular subject for drug development research. Studies on the development of drugs for AD have primarily concentrated on the use of multitarget directed ligands. Following this strategy, we designed new ChE inhibitors with additional antioxidant and metal chelator effects. In this research, eight novel N’‐(quinolin‐4‐ylmethylene)propanehydrazide derivatives were synthesized and characterized. We then evaluated the inhibition potency of all the final compounds for cholinesterase enzymes. Among them, 4e (IC50 acetylcholinesterase [AChE] = 0.69 µM and butyrylcholinesterase [BChE]= 26.00 µM) and 4h (IC50's AChE= 7.04 µM and BChE= 16.06 µM) were found to be the most potent AChE and BChE inhibitors, respectively.