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, 16 (3), 1431-43

Design, Synthesis and Preliminary Pharmacological Evaluation of New Piperidine and Piperazine Derivatives as Cognition-Enhancers

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Design, Synthesis and Preliminary Pharmacological Evaluation of New Piperidine and Piperazine Derivatives as Cognition-Enhancers

Elisabetta Martini et al. Bioorg Med Chem.

Abstract

A series of 2-oxopiperazine, 4-aminomethyl-, 3-amino- and 3-aminomethylpiperidine analogues of DM235 (sunifiram) and MN19 (sapunifiram), two previously reported potent cognition-enhancers, have been synthesized and tested in the mouse passive-avoidance test. The compounds display minimal effective doses in the range 0.3-10mg/kg. Although the new substances do not show improved activity when compared to the parent compounds, some useful information has been obtained to understand structure-activity relationships. In addition, the 3-aminopiperidine moiety appears to be a promising scaffold to synthesize new drugs endowed with cognition-enhancing activity.

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