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Elsevier, European Journal of Medicinal Chemistry, 10(45), p. 4490-4498

DOI: 10.1016/j.ejmech.2010.07.009

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Synthesis of new 3-aryl-4,5-dihydropyrazole-1-carbothioamide derivatives. An investigation on their ability to inhibit monoamine oxidase

Journal article published in 2010 by E. Maccioni, S. Alcaro, F. Orallo, M. C. Cardia, S. Distinto, G. Costa ORCID, M. Yanez, M. L. Sanna, S. Vigo, R. Meleddu, D. Secci
This paper was not found in any repository, but could be made available legally by the author.
This paper was not found in any repository, but could be made available legally by the author.

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Abstract

Some differently substituted 3-aryl-4,5-dihydropyrazoles-1-carbothioamides have been synthesised with the aim to investigate their monoamine oxidase inhibitory activity. The chemical structures of the compounds have been characterized by means of their IR. (1)H NMR, (13)C NMR spectroscopic data and elemental analyses. All the active compounds showed a selective activity towards the B isoform of the enzyme, regardless of the substitution on the heterocyclic ring The inhibition of the enzymatic activity was measured on human recombinant MAO isoforms, expressed in baculovirus infected BTI insect cells. Docking experiments were carried out with the aim to rationalize the mechanism of inhibition of the most active and selective compound. (C) 2010 Elsevier Masson SAS. All rights reserved.