A series of amides, structurally related to DM232 (unifiram) and DM235 (sunifiram), characterized by a 1,2,3,4-tetrahydropyrazino[2,1-a]isoindol-6(2H)-one, 1,4-diamino-cyclohexane or 1,4-diaminobenzene ring, have been synthesized and tested for cognition-enhancing activity in the mouse passive-avoidance test. Some of the compounds display good antiamnesic and procognitive activity, with higher potency than piracetam, while some cyclohexane derivatives are endowed with amnesia inducing properties.
Design, synthesis and preliminary pharmacological evaluation of new analogues of DM232 (unifiram) and DM235 (sunifiram) as cognition modulators / Martini, Elisabetta; Norcini, Monica; Ghelardini, Carla; Manetti, Dina; Dei, Silvia; Guandalini, Luca; Melchiorre, Michele; Pagella, Simona; Scapecchi, Serena; Teodori, Elisabetta; Romanelli, MARIA NOVELLA. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 1464-3391. - STAMPA. - 16:(2008), pp. 10034-10042. [10.1016/j.bmc.2008.10.017]
Design, synthesis and preliminary pharmacological evaluation of new analogues of DM232 (unifiram) and DM235 (sunifiram) as cognition modulators.
MARTINI, ELISABETTA;NORCINI, MONICA;GHELARDINI, CARLA;MANETTI, DINA;DEI, SILVIA;GUANDALINI, LUCA;MELCHIORRE, MICHELE;PAGELLA, SIMONA;SCAPECCHI, SERENA;TEODORI, ELISABETTA;ROMANELLI, MARIA NOVELLA
2008
Abstract
A series of amides, structurally related to DM232 (unifiram) and DM235 (sunifiram), characterized by a 1,2,3,4-tetrahydropyrazino[2,1-a]isoindol-6(2H)-one, 1,4-diamino-cyclohexane or 1,4-diaminobenzene ring, have been synthesized and tested for cognition-enhancing activity in the mouse passive-avoidance test. Some of the compounds display good antiamnesic and procognitive activity, with higher potency than piracetam, while some cyclohexane derivatives are endowed with amnesia inducing properties.File | Dimensione | Formato | |
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