Bioorganic & Medicinal Chemistry 2004-01-02

Structure-activity relationship studies on unifiram (DM232) and sunifiram (DM235), two novel and potent cognition enhancing drugs.

Serena Scapecchi, Elisabetta Martini, Dina Manetti, Carla Ghelardini, Cecilia Martelli, Silvia Dei, Nicoletta Galeotti, Luca Guandalini, Maria Novella Romanelli, Elisabetta Teodori

Index: Bioorg. Med. Chem. 12(1) , 71-85, (2004)

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Abstract

Structure-activity relationships on two novel potent cognition enhancing drugs, unifiram (DM232, 1) and sunifiram (DM235, 2), are reported. Although none of the compounds synthesised reached the potency of the parent drugs, some fairly active compounds have been identified that may represent new leads to develop other cognition enhancing drugs. An interesting result of this research is the identification of two compounds (13 and 14) that are endowed with amnesing activity (the opposite of the activity of the original molecules) and are nearly equipotent to scopolamine. Moreover, two compounds of the series (5 and 6) were found endowed with analgesic activity on a rat model of neuropathic pain at the dose of 1 mg/kg.