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

• Main Authors: Maria Paola Giovannoni (Author), Igor A. Schepetkin (Author), Mark T. Quinn (Author), Niccolò Cantini (Author), Letizia Crocetti (Author), Gabriella Guerrini (Author), Antonella Iacovone (Author), Paola Paoli (Author), Patrizia Rossi (Author), Gianluca Bartolucci (Author), Marta Menicatti (Author), Claudia Vergelli (Author)
• Format: Book
• Published: Taylor & Francis Group, 2018-01-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

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...