Synthesis and selective inhibition of human monoamine oxidases of a large scaffold of (4,5-substituted-thiazol-2-yl)hydrazones†,10.1039/C0MD00014K

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Lactoyl-CoA 全氟丁基戊烷白叶藤碱全氟己基辛烷新白叶藤碱壳寡糖特色专题-生物多肽

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

Franco Chimenti,Daniela Secci,Adriana Bolasco,Paola Chimenti,Arianna Granese,Simone Carradori,Melissa D'Ascenzio,Matilde Yáñez,Francisco Orallo

MedChemComm Pub Date : 04/28/2010 00:00:00 , DOI:10.1039/C0MD00014K

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.