Structure-activity relationship studies on unifiram (DM232) and sunifiram (DM235), two novel and potent cognition enhancing drugs.
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.
Scapecchi
Serena
S
Dipartimento di Scienze Farmaceutiche, Università di Firenze, Via G. Capponi 9, I-50121, Firenze, Italy. fulvio.gualtieri@unifi.it
Martini
Elisabetta
E
Manetti
Dina
D
Ghelardini
Carla
C
Martelli
Cecilia
C
Dei
Silvia
S
Galeotti
Nicoletta
N
Guandalini
Luca
L
Novella Romanelli
Maria
M
Teodori
Elisabetta
E
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
D018697:Nootropic Agents; D010879:Piperazines; D011758:Pyrroles; C416655:DM 235; C409868:DM 232