Format

Send to

Choose Destination
J Med Chem. 2006 Jun 1;49(11):3421-5.

Discovery of huperzine A-tacrine hybrids as potent inhibitors of human cholinesterases targeting their midgorge recognition sites.

Author information

1
Dipartimento Farmaco Chimico Tecnologico, Via Aldo Moro, Universita' di Siena, 53100 Siena, Italy.

Abstract

We describe herein the development of novel huperzine A-tacrine hybrids characterized by 3-methylbicyclo[3.3.1]non-3-ene scaffolds. These compounds were specifically designed to establish tight interactions, through different binding modes, with the midgorge recognition sites of human acetylcholinesterase (hAChE: Y72, D74) and human butyrylcholinesterase (hBuChE: N68, D70) and their catalytic or peripheral sites. Compounds 5a-c show a markedly improved biological profile relative to tacrine and huperzine A.

PMID:
16722663
DOI:
10.1021/jm060257t
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for American Chemical Society
Loading ...
Support Center