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Optimization of O3-Acyl Kojic Acid Derivatives as Potent and SelectiveHuman Neutrophil Elastase Inhibitors.
- Source :
-
Journal of Medicinal Chemistry . Dec2013, Vol. 56 Issue 23, p9802-9806. 5p. - Publication Year :
- 2013
-
Abstract
- Humanneutrophil elastase (HNE) is an attractive target for treating chronicand acute inflammatory lung diseases. An optimization campaign ofthe kojic acid scaffold to develop new potent HNE inhibitors is reported. O3-Pivaloyl derivatives were shown to be themost potent inhibitors with IC5ovalues down to 80 nM.These compounds presented excellent selectivity and cytotoxicity profileswith suitable ligand efficiency. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 00222623
- Volume :
- 56
- Issue :
- 23
- Database :
- Academic Search Index
- Journal :
- Journal of Medicinal Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 92984923
- Full Text :
- https://doi.org/10.1021/jm4011725