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.

Structure-activity relationship studies on unifiram (DM232) and sunifiram (DM235), two novel and potent cognition enhancing drugs / S. SCAPECCHI; E. MARTINI; D. MANETTI; C. GHELARDINI; C. MARTELLI; S. DEI; N. GALEOTTI; L. GUANDALINI; M. ROMANELLI; E. TEODORI. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - STAMPA. - 12(2004), pp. 71-85. [10.1016/j.bmc.2003.10.025]

Structure-activity relationship studies on unifiram (DM232) and sunifiram (DM235), two novel and potent cognition enhancing drugs

SCAPECCHI, SERENA;MARTINI, ELISABETTA;MANETTI, DINA;GHELARDINI, CARLA;MARTELLI, CECILIA;DEI, SILVIA;GALEOTTI, NICOLETTA;GUANDALINI, LUCA;ROMANELLI, MARIA NOVELLA;TEODORI, ELISABETTA
2004

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.
12
71
85
S. SCAPECCHI; E. MARTINI; D. MANETTI; C. GHELARDINI; C. MARTELLI; S. DEI; N. GALEOTTI; L. GUANDALINI; M. ROMANELLI; E. TEODORI
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/2158/307734
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