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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 IC(50) val...

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Detalles Bibliográficos
Autores principales: Giovannoni, Maria Paola, Schepetkin, Igor A., Quinn, Mark T., Cantini, Niccolò, Crocetti, Letizia, Guerrini, Gabriella, Iacovone, Antonella, Paoli, Paola, Rossi, Patrizia, Bartolucci, Gianluca, Menicatti, Marta, Vergelli, Claudia
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6032016/
https://www.ncbi.nlm.nih.gov/pubmed/29969929
http://dx.doi.org/10.1080/14756366.2018.1480615