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 0.3–10 mg/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.
Design, synthesis and preliminary pharmacological evaluation of new piperidine and piperazine derivatives as cognition-enhancers / Martini, Elisabetta; Ghelardini, Carla; Dei, Silvia; Guandalini, Luca; Manetti, Dina; Melchiorre, Michele; Norcini, Monica; Scapecchi, Serena; Teodori, Elisabetta; Romanelli, MARIA NOVELLA. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 1464-3391. - STAMPA. - 16:(2008), pp. 1431-1443. [10.1016/j.bmc.2007.10.050]
Design, synthesis and preliminary pharmacological evaluation of new piperidine and piperazine derivatives as cognition-enhancers
MARTINI, ELISABETTA;GHELARDINI, CARLA;DEI, SILVIA;GUANDALINI, LUCA;MANETTI, DINA;MELCHIORRE, MICHELE;NORCINI, MONICA;SCAPECCHI, SERENA;TEODORI, ELISABETTA;ROMANELLI, MARIA NOVELLA
2008
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 0.3–10 mg/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.File | Dimensione | Formato | |
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