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Your search keyword '"Correia, Henrique F."' showing total 2 results
Start Over Author "Correia, Henrique F." Publisher american chemical society
2 results on '"Correia, Henrique F."'

2. Optimization of O3-acyl kojic acid derivatives as potent and selective human neutrophil elastase inhibitors.

Author

Lucas SD, Gonçalves LM, Carvalho LA, Correia HF, Da Costa EM, Guedes RA, Moreira R, and Guedes RC

Subjects
Animals, Cell Line, Drug Stability, Humans, Inhibitory Concentration 50, Kinetics, Microsomes, Liver metabolism, Molecular Docking Simulation, Proteinase Inhibitory Proteins, Secretory pharmacology, Pyridones chemical synthesis, Pyridones pharmacology, Rats, Structure-Activity Relationship, Leukocyte Elastase metabolism, Proteinase Inhibitory Proteins, Secretory chemical synthesis, Pyrones chemistry
Abstract

Human neutrophil elastase (HNE) is an attractive target for treating chronic and acute inflammatory lung diseases. An optimization campaign of the kojic acid scaffold to develop new potent HNE inhibitors is reported. O3-Pivaloyl derivatives were shown to be the most potent inhibitors with IC5o values down to 80 nM. These compounds presented excellent selectivity and cytotoxicity profiles with suitable ligand efficiency.

Published
2013
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