Synthesis, biological evaluation, and molecular modelling studies of potent human neutrophil elastase (HNE) inhibitors

We report the synthesis and biological evaluation of a new series of 3- or 4-(substituted)phenylisoxazolones as HNE inhibitors. Due to tautomerism of the isoxazolone nucleus, two isomers were obtained as final compounds (2-NCO and 5-OCO) and the 2-NCO derivatives were the most potent with IC50 value...

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Autori principali: Maria Paola Giovannoni, Igor A. Schepetkin, Mark T. Quinn, Niccolò Cantini, Letizia Crocetti, Gabriella Guerrini, Antonella Iacovone, Paola Paoli, Patrizia Rossi, Gianluca Bartolucci, Marta Menicatti, Claudia Vergelli
Natura: Artigo
Lingua:Inglês
Pubblicazione: Taylor & Francis Group 2018-01-01
Serie:Journal of Enzyme Inhibition and Medicinal Chemistry
Soggetti:
Isoxazol-5(2H)-one
HNE
molecular modelling
stability
Accesso online:http://dx.doi.org/10.1080/14756366.2018.1480615
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