title: Synthesis and cholinesterase inhibitory activity of 6-, 7-methoxy-(and hydroxy-) tacrine derivatives.
abstract: Some 6- and 7-methoxy-(and hydroxy-) tacrine derivatives were synthesized and evaluated for their in vitro acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities. The most potent analogue in our series was the 9-heptylamino-6-methoxytacrine 3af which, in comparison with tacrine (THA), displayed an almost identical inhibitory effect, slightly lower acute toxicity and higher selectivity profile towards AchE when compared with THA.
authors.affiliation: Laboratorio di Chimica del Farmaco, Istituto Superiore di Sanità, Roma, Italy.
authors.forename: M R
authors.initials: MR
authors.lastname: Del Giudice
authors.forename: A
authors.initials: A
authors.lastname: Borioni
authors.forename: C
authors.initials: C
authors.lastname: Mustazza
authors.forename: F
authors.initials: F
authors.lastname: Gatta
authors.forename: A
authors.initials: A
authors.lastname: Meneguz
authors.forename: M T
authors.initials: MT
authors.lastname: Volpe
mesh_terms: D000818:Animals; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D008297:Male; D051379:Mice; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship; D013619:Tacrine / Q000031:analogs & derivatives*
chemical_list: D002800:Cholinesterase Inhibitors; D013619:Tacrine