Journal
JOURNAL OF PINEAL RESEARCH
Volume 54, Issue 4, Pages 435-441Publisher
WILEY
DOI: 10.1111/jpi.12006
Keywords
Alzheimer's disease; cholinesterases inhibitors; hybrid drugs
Categories
Funding
- National Science Center [2011/03/B/ST5/01593]
Ask authors/readers for more resources
Novel inhibitors of cholinesterases, especially butyrylcholinesterase (BuChE), were obtained by coupling melatonin-tacrine heterodimers via the carbamate bond. Compounds 14a-i possessed potent cholinesterase inhibitory activity (with IC50 values as low as 1.18nm for acetylcholinesterase (AChE) and 0.24nm 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 tacrine 4.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available