New β-arylchalcogeno amines with procognitive properties targeting Carbonic Anhydrases and Monoamine Oxidases.
Journal: European journal of medicinal chemistry
Volume: 244
Issue:
Year of Publication: 2022
Affiliated Institutions:
Department of Neuroscience, Psychology, Drug Research and Child Health (NEUROFARBA), University of Florence, Viale G. Pieraccini , , Florence, Italy. Electronic address: gustavo.provensi@unifi.it.
Department of Health Sciences, University of Florence, Viale Pieraccini Florence, Florence, Italy.
Department of Chemistry "Ugo Schiff", University of Florence, Via Della Lastruccia -, I-, Sesto Fiorentino, Italy.
Department of Pharmacy, "G. D'Annunzio" University of Chieti-Pescara, Via Dei Vestini , , Chieti, Italy.
Pharmaceutical Chemistry and Centre of Excellence for Pharmaceutical Sciences, North-West University, Private Bag X, Potchefstroom, , South Africa.
NEUROFARBA Department, Sezione di Scienze Farmaceutiche, University of Florence, Via Ugo Schiff , , Sesto Fiorentino, Florence, Italy.
Department of Food and Drug, University of Parma, Parco Area Delle Scienze, /A, , Parma, Italy.
Department of Neuroscience, Psychology, Drug Research and Child Health (NEUROFARBA), University of Florence, Viale G. Pieraccini , , Florence, Italy.
NEUROFARBA Department, Sezione di Scienze Farmaceutiche, University of Florence, Via Ugo Schiff , , Sesto Fiorentino, Florence, Italy; Department of Food and Drug, University of Parma, Parco Area Delle Scienze, /A, , Parma, Italy. Electronic address: andrea.angeli@unifi.it.
Abstract summary
Cognitive deficits are enduring and disabling symptoms for many patients with severe mental illness, and these impairments are inadequately addressed by current medications. In this study, we reported the synthesis of β-arylchalcogeno amines bearing sulfurated, selenated, and tellurated moieties (2-4) which are structurally related to amphetamine with good activation properties for Carbonic Anhydrases (CAs) isoforms present in the cortical and hippocampal brain structures (hCA IV and hCA XIV). In addition, these compounds showed selective inhibition against the Monoamine oxidase (MAO) A isoform. In vivo evaluation of two derivatives (2a and 3a) revealed procognitive effects in the object recognition and social discrimination tests. Interestingly, these compounds, despite having a similar structure to amphetamine, did not caused hypophagia or hyperlocomotion, two effects often observed following the administration of amphetamine-like drugs. In this context, β-arylchalcogeno amines may have utility for improving the symptoms of cognitive decline associated with neurodegenerative and psychiatric diseases such as attention deficit disorder, Parkinson's disease-related cognitive dysfunction and cognitive disorders associated with depression.
Authors & Co-authors:
Provensi Gustavo G
Costa Alessia A
Rani Barbara B
Becagli Maria Vittoria MV
Vaiano Fabio F
Passani Maria Beatrice MB
Tanini Damiano D
Capperucci Antonella A
Carradori Simone S
Petzer Jacobus P JP
Petzer Anél A
Vullo Daniela D
Costantino Gabriele G
Blandina Patrizio P
Angeli Andrea A
Supuran Claudiu T CT
Study Outcome
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