Design, synthesis and nootropic activity of new analogues of sunifiram and sapunifiram, two potent cognition-enhancers

Elisabetta Martini; Alberto Salvicchi; Carla Ghelardini; Dina Manetti; Silvia Dei; Luca Guandalini; Cecilia Martelli; Michele Melchiorre; Cristina Cellai; Serena Scapecchi; Elisabetta Teodori; Maria Novella Romanelli

doi:10.1016/j.bmc.2009.08.055

Design, synthesis and nootropic activity of new analogues of sunifiram and sapunifiram, two potent cognition-enhancers

Bioorg Med Chem. 2009 Nov 1;17(21):7606-14. doi: 10.1016/j.bmc.2009.08.055. Epub 2009 Sep 3.

Authors

Elisabetta Martini¹, Alberto Salvicchi, Carla Ghelardini, Dina Manetti, Silvia Dei, Luca Guandalini, Cecilia Martelli, Michele Melchiorre, Cristina Cellai, Serena Scapecchi, Elisabetta Teodori, Maria Novella Romanelli

Affiliation

¹ Department of Pharmaceutical Sciences, Laboratory of Design, Synthesis and Study of Biologically Active Heterocycles (HeteroBioLab), University of Florence, 50019 Sesto Fiorentino, Italy.

PMID: 19786353
DOI: 10.1016/j.bmc.2009.08.055

Abstract

A series of amides and sulfonamides, structurally related to DM235 (sunifiram) and MN19 (sapunifiram), derived by ring expansion or contraction, or by inversion of the exocyclic amide function, 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, and with a potency similar to the parent compounds.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Cognition / drug effects*
Disease Models, Animal
Drug Design
Mice
Nootropic Agents / chemical synthesis*
Nootropic Agents / chemistry
Nootropic Agents / pharmacology
Piperazines / chemical synthesis*
Piperazines / chemistry*
Piperazines / pharmacology
Sulfonamides / chemical synthesis*
Sulfonamides / chemistry
Sulfonamides / pharmacology

Substances

Nootropic Agents
Piperazines
Sulfonamides
sapunifiram
DM 235