Format

Send to

Choose Destination
J Med Chem. 2013 Dec 12;56(23):9802-6. doi: 10.1021/jm4011725. Epub 2013 Nov 20.

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

Author information

1
Instituto de Investigação do Medicamento (iMed.ULisboa), Faculdade de Farmácia, Universidade de Lisboa , Av. Prof. Gama Pinto, 1649-003 Lisboa, Portugal.

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.

PMID:
24224573
DOI:
10.1021/jm4011725
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for American Chemical Society
Loading ...
Support Center