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 IC 50 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. © 2011 The Royal Society of Chemistry.
Synthesis and selective inhibition of human monoamine oxidases of a large scaffold of (4,5-substituted-thiazol-2-yl)hydrazones / Chimenti, Franco; Secci, Daniela; Chimenti, Paola; Granese, Arianna; Carradori, Simone; D'Ascenzio, Melissa; Matilde, Yanez; Francisco, Orallo; Bolasco, Adriana. - In: MEDCHEMCOMM. - ISSN 2040-2503. - 1:1(2010), pp. 61-72. [10.1039/c0md00014k]
Synthesis and selective inhibition of human monoamine oxidases of a large scaffold of (4,5-substituted-thiazol-2-yl)hydrazones
CHIMENTI, Franco;SECCI, DANIELA;CHIMENTI, Paola;Arianna Granese;CARRADORI, Simone;D'ASCENZIO, MELISSA;BOLASCO, Adriana
2010
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 IC 50 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. © 2011 The Royal Society of Chemistry.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
