2. Academic Validation
  3. Design, synthesis and preliminary pharmacological evaluation of new analogues of DM232 (unifiram) and DM235 (sunifiram) as cognition modulators

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

Affiliation

  • 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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