Potent, easily synthesized huperzine A-tacrine hybrid acetylcholinesteraseinhibitors

Authors
Carlier, PR Du, DM Han, YF Liu, J Pang, YP
Citation
Pr. Carlier et al., Potent, easily synthesized huperzine A-tacrine hybrid acetylcholinesteraseinhibitors, BIOORG MED, 9(16), 1999, pp. 2335-2338
Citations number
13
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
16
Year of publication
1999
Pages
2335 - 2338
Database
ISI
SICI code
0960-894X(19990816)9:16<2335:PESHAH>2.0.ZU;2-L
Abstract
Hybrid acetylcholinesterase inhibitors composed of a key fragment of huperz ine A and an intact tacrine unit were prepared. The syntheses are quite dir ect, proceeding in a maximum of 4 linear steps from commercially available starting materials. The optimum hybrid inhibitor (+/-)-9g is 13-fold more p otent than (-)-huperzine A, and 25-fold more potent than tacrine. (C) 1999 Elsevier Science Ltd. All rights reserved.