Bioorg Med Chem. 2008 Dec 1;16(23):10034-42. Epub 2008 Oct 11.

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

Martini E, Norcini M, Ghelardini C, Manetti D, Dei S, Guandalini L, Melchiorre M, Pagella S, Scapecchi S, Teodori E, Romanelli MN.

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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.

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.

PMID:: 18954993; [PubMed - indexed for MEDLINE]

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