Issue 1, 2010
From the journal:

MedChemComm

Synthesis and selective inhibition of human monoamine oxidases of a large scaffold of (4,5-substituted-thiazol-2-yl)hydrazones†

Franco Chimenti,a   Daniela Secci,*a   Adriana Bolasco,a   Paola Chimenti,a   Arianna Granese,a   Simone Carradori,a   Melissa D'Ascenzio,a   Matilde Yáñezb  and  Francisco Orallob  

* Corresponding authors

a Dipartimento di Chimica e Tecnologie del Farmaco, Università degli Studi di Roma “La Sapienza”, P.le A. Moro 5, 00185 Rome, Italy
E-mail: daniela.secci@uniroma1.it
Fax: +39 06 49913772
Tel: +39 06 49913149

b Departamento de Farmacología and Instituto de Farmacia Industrial, Facultad de Farmacia, Universidad de Santiago de Compostela, Campus Universitario Sur, E-15782 Santiago de Compostela, La Coruña, Spain

Abstract

A large class of (4,5-substituted-thiazol-2-yl)hydrazone derivatives (1–66) was synthesized in good yield (82–99%) and characterized by elemental analysis and 1H NMR studies. The compounds were assayed for their in vitro human monoamine oxidase inhibitory activity and selectivity. Most of them showed IC50 values in the micromolar range. Our aim was to evaluate the importance of a bulky group at C2, C4, and C5 positions of the thiazole nucleus in modulating the biological activity of this scaffold.

Graphical abstract: Synthesis and selective inhibition of human monoamine oxidases of a large scaffold of (4,5-substituted-thiazol-2-yl)hydrazones

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Article information

DOI
https://doi.org/10.1039/C0MD00014K
Article type
Concise Article
Submitted
18 Feb 2010
Accepted
21 Mar 2010
First published
28 Apr 2010

Med. Chem. Commun., 2010,1, 61-72

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Synthesis and selective inhibition of human monoamine oxidases of a large scaffold of (4,5-substituted-thiazol-2-yl)hydrazones

F. Chimenti, D. Secci, A. Bolasco, P. Chimenti, A. Granese, S. Carradori, M. D'Ascenzio, M. Yáñez and F. Orallo, Med. Chem. Commun., 2010, 1, 61 DOI: 10.1039/C0MD00014K

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