title: Design, synthesis and preliminary pharmacological evaluation of new piperidine and piperazine derivatives as cognition-enhancers.
abstract: A series of 2-oxopiperazine, 4-aminomethyl-, 3-amino- and 3-aminomethylpiperidine analogues of DM235 (sunifiram) and MN19 (sapunifiram), two previously reported potent cognition-enhancers, have been synthesized and tested in the mouse passive-avoidance test. The compounds display minimal effective doses in the range 0.3-10mg/kg. Although the new substances do not show improved activity when compared to the parent compounds, some useful information has been obtained to understand structure-activity relationships. In addition, the 3-aminopiperidine moiety appears to be a promising scaffold to synthesize new drugs endowed with cognition-enhancing activity.
authors.affiliation: Laboratory of Design, Synthesis and Study of Biologically Active Heterocycles (HeteroBioLab), Department of Pharmaceutical Sciences, University of Florence, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Italy.
authors.forename: Elisabetta
authors.initials: E
authors.lastname: Martini
authors.forename: Carla
authors.initials: C
authors.lastname: Ghelardini
authors.forename: Silvia
authors.initials: S
authors.lastname: Dei
authors.forename: Luca
authors.initials: L
authors.lastname: Guandalini
authors.forename: Dina
authors.initials: D
authors.lastname: Manetti
authors.forename: Michele
authors.initials: M
authors.lastname: Melchiorre
authors.forename: Monica
authors.initials: M
authors.lastname: Norcini
authors.forename: Serena
authors.initials: S
authors.lastname: Scapecchi
authors.forename: Elisabetta
authors.initials: E
authors.lastname: Teodori
authors.forename: Maria Novella
authors.initials: MN
authors.lastname: Romanelli
mesh_terms: D000215:Acylation; D000818:Animals; D003071:Cognition / Q000187:drug effects*; D015195:Drug Design; D051379:Mice; D015394:Molecular Structure; D010880:Piperidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013455:Sulfur / Q000737:chemistry
chemical_list: D010880:Piperidines; C032727:piperidine; D013455:Sulfur