Journal
ARCHIV DER PHARMAZIE
Volume 345, Issue 8, Pages 591-597Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ardp.201200018
Keywords
Acetylcholinesterase inhibitors; Butyrylcholinesterase inhibitors; Derivatives of piperidine and homopiperidine; Histamine H3 receptor; Multifunctional ligands; Non-imidazole ligands of H3 receptor
Funding
- Ministry of Science and Higher Education [K/ZDS/001915]
- FP7 EU COST Actions [BM0806]
Ask authors/readers for more resources
The study presents novel biological properties of diether derivatives of homo- or substituted piperidine ligands of the histamine H3 receptor. The compounds were evaluated for their inhibitory potency against acetylcholinesterase (AChE) from the electric eel and butyrylcholinesterase (BuChE) from horse serum. The most interesting multifunctional compound 13 displayed high affinity for the cloned hH3R (Ki?=?3.48?nM) and moderate inhibitory potency against both enzymes (IC50 AChE?=?7.91?mu M and BuChE?=?4.97?mu M). Molecular modeling studies revealed interactions with key amino acid residues in the homology model of histamine H3 receptor ligands, as well as the binding model for AChE and BuChE in the catalytic and peripheral active sites.
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