Design, synthesis and preliminary pharmacological evaluation of new analogues of DM232 (unifiram) and DM235 (sunifiram) as cognition modulators

  • Bioorg Med Chem. 2008 Dec 1;16(23):10034-42. doi: 10.1016/j.bmc.2008.10.017.
Elisabetta Martini  1 ,  Monica Norcini ,  Carla Ghelardini ,  Dina Manetti ,  Silvia Dei ,  Luca Guandalini ,  Michele Melchiorre ,  Simona Pagella ,  Serena Scapecchi ,  Elisabetta Teodori ,  Maria Novella Romanelli
Affiliations
  • 1. 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.
PMID: 18954993 DOI: 10.1016/j.bmc.2008.10.017
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.

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