Investigations on the 2-thiazolylhydrazyne scaffold: Synthesis and molecular modeling of selective human monoamine oxidase inhibitors

…, P Chimenti, A Granese, S Carradori, M Yáñez…

Index: Chimenti, Franco; Bolasco, Adriana; Secci, Daniela; Chimenti, Paola; Granese, Arianna; Carradori, Simone; Yanez, Matilde; Orallo, Francisco; Ortuso, Francesco; Alcaro, Stefano Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 15 p. 5715 - 5723

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Citation Number: 48

Abstract

A new series of [4-(3-methoxyphenyl)-thiazol-2-yl] hydrazyne derivatives were synthesized in good yield (71–99%) and characterized by elemental analysis and 1H NMR studies. The compounds were assayed for their in vitro human monoamine oxidase (hMAO) inhibitory activity and selectivity and most of them showed IC50 values in the nanomolar range, thus demonstrating our interest in this privileged scaffold. The most active and selective ...