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

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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Bibliographic Details
Main Authors: 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
Format: Article
Language:English
Published: Taylor & Francis Group 2018-01-01
Series:Journal of Enzyme Inhibition and Medicinal Chemistry
Subjects:
Isoxazol-5(2H)-one
HNE
molecular modelling
stability
Online Access:http://dx.doi.org/10.1080/14756366.2018.1480615

Internet

http://dx.doi.org/10.1080/14756366.2018.1480615

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