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.
2008
16
10034
10042
Martini, Elisabetta; Norcini, Monica; Ghelardini, Carla; Manetti, Dina; Dei, Silvia; Guandalini, Luca; Melchiorre, Michele; Pagella, Simona; Scapecchi...espandi
File in questo prodotto:
File Dimensione Formato  
Martini Bioorg 08 II.pdf

Accesso chiuso

Tipologia: Altro
Licenza: Tutti i diritti riservati
Dimensione 300.42 kB
Formato Adobe PDF
300.42 kB Adobe PDF   Richiedi una copia

I documenti in FLORE sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificatore per citare o creare un link a questa risorsa: https://hdl.handle.net/2158/354654
Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus 13
  • ???jsp.display-item.citation.isi??? 12
social impact