| Literature DB >> 24224573 |
Susana D Lucas1, Lídia M Gonçalves, Luís A R Carvalho, Henrique F Correia, Eduardo M R Da Costa, Romina A Guedes, Rui Moreira, Rita C Guedes.
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.Entities:
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Year: 2013 PMID： 24224573 DOI： 10.1021/jm4011725
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446