title: Potent, easily synthesized huperzine A-tacrine hybrid acetylcholinesterase inhibitors.
abstract: Hybrid acetylcholinesterase inhibitors composed of a key fragment of huperzine A and an intact tacrine unit were prepared. The syntheses are quite direct, proceeding in a maximum of 4 linear steps from commercially available starting materials. The optimum hybrid inhibitor (+/-)-9g is 13-fold more potent than (-)-huperzine A, and 25-fold more potent than tacrine.
authors.affiliation: Department of Chemistry, Hong Kong University of Science and Technology, Clear Water Bay, Kowloon. chpaul@ust.hk
authors.forename: P R
authors.initials: PR
authors.lastname: Carlier
authors.forename: D M
authors.initials: DM
authors.lastname: Du
authors.forename: Y
authors.initials: Y
authors.lastname: Han
authors.forename: J
authors.initials: J
authors.lastname: Liu
authors.forename: Y P
authors.initials: YP
authors.lastname: Pang
mesh_terms: D000110:Acetylcholinesterase / Q000187:drug effects*; D000470:Alkaloids; D002800:Cholinesterase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D012717:Sesquiterpenes / Q000737:chemistry*; D013619:Tacrine / Q000737:chemistry*
chemical_list: D000470:Alkaloids; D002800:Cholinesterase Inhibitors; D012717:Sesquiterpenes; C050426:huperzine A; D013619:Tacrine; D000110:Acetylcholinesterase