title: Structure-activity relationship studies on unifiram (DM232) and sunifiram (DM235), two novel and potent cognition enhancing drugs.
abstract: Structure-activity relationships on two novel potent cognition enhancing drugs, unifiram (DM232, 1) and sunifiram (DM235, 2), are reported. Although none of the compounds synthesised reached the potency of the parent drugs, some fairly active compounds have been identified that may represent new leads to develop other cognition enhancing drugs. An interesting result of this research is the identification of two compounds (13 and 14) that are endowed with amnesing activity (the opposite of the activity of the original molecules) and are nearly equipotent to scopolamine. Moreover, two compounds of the series (5 and 6) were found endowed with analgesic activity on a rat model of neuropathic pain at the dose of 1 mg/kg.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Firenze, Via G. Capponi 9, I-50121, Firenze, Italy. fulvio.gualtieri@unifi.it
authors.forename: Serena
authors.initials: S
authors.lastname: Scapecchi
authors.forename: Elisabetta
authors.initials: E
authors.lastname: Martini
authors.forename: Dina
authors.initials: D
authors.lastname: Manetti
authors.forename: Carla
authors.initials: C
authors.lastname: Ghelardini
authors.forename: Cecilia
authors.initials: C
authors.lastname: Martelli
authors.forename: Silvia
authors.initials: S
authors.lastname: Dei
authors.forename: Nicoletta
authors.initials: N
authors.lastname: Galeotti
authors.forename: Luca
authors.initials: L
authors.lastname: Guandalini
authors.forename: Maria
authors.initials: M
authors.lastname: Novella Romanelli
authors.forename: Elisabetta
authors.initials: E
authors.lastname: Teodori
mesh_terms: D000818:Animals; D001362:Avoidance Learning / Q000187:drug effects / Q000502:physiology; D004305:Dose-Response Relationship, Drug; D051379:Mice; D018697:Nootropic Agents / Q000737:chemistry* / Q000494:pharmacology; D010147:Pain Measurement / Q000187:drug effects / Q000379:methods; D017288:Pain Threshold / Q000187:drug effects; D010879:Piperazines / Q000737:chemistry* / Q000494:pharmacology; D011758:Pyrroles / Q000737:chemistry* / Q000494:pharmacology; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D018697:Nootropic Agents; D010879:Piperazines; D011758:Pyrroles; C416655:DM 235; C409868:DM 232