Highly selective inhibition of butyrylcholinesterase by a novel melatonin–tacrine heterodimers. Issue 4 (May 2013)

• Record Type: Journal Article
• Authors: Zawadzka, Anna; Łozińska, Iwona; Molęda, Zuzanna; Panasiewicz, Mirosława; Czarnocki, Zbigniew
• Is Part Of: Journal of pineal research. Volume 54:Issue 4(2013)
• Page Start: 435
• Page End: 441
• Publication Date: 2013-05
• Subjects: Alzheimer's disease -- cholinesterases inhibitors -- hybrid drugs; Pineal gland -- Periodicals; Pineal Gland -- Periodicals; Épiphyse (Glande); Périodique électronique (Descripteur de forme); Ressource Internet (Descripteur de forme); 612.492
• DOI: 10.1111/jpi.12006
• Languages: English
• ISSNs: 0742-3098

Abstract

Abstract: Novel inhibitors of cholinesterases, especially butyrylcholinesterase (BuChE), were obtained by coupling melatonin–tacrine heterodimers via the carbamate bond. Compounds14a‐i possessed potent cholinesterase inhibitory activity (with IC50 values as low as 1.18 nm for acetylcholinesterase (AChE) and 0.24 nm for butyrylcholinesterase (BuChE)). These heterodimers exhibit selectivity toward BuChE, being from 4‐ to 256‐fold more active toward BuChE than AChE, but still acting as better AChE inhibitors than tacrine4 .