73825-96-4Relevant articles and documents
2-(2-Oxo-morpholin-3-yl)-acetamide derivatives as broad-spectrum antifungal agents
Bardiot, Dorothée,Thevissen, Karin,De Brucker, Katrijn,Peeters, Annelies,Cos, Paul,Taborda, Carlos P.,McNaughton, Michael,Maes, Louis,Chaltin, Patrick,Cammue, Bruno P. A.,Marchand, Arnaud
, p. 1502 - 1512 (2015/03/04)
From a fungicidal screen, we identified 2-(2-oxo-morpholin-3-yl)-acetamide derivatives as fungicidal agents against Candida species, additionally characterized by antifungal activity against Aspergillus species. However, development of this series was hampered by low plasmatic stability. Introduction of a gem-dimethyl on the 6-position of the morpholin-2-one core led to considerable improvement in plasmatic stability while maintaining in vitro antifungal activity. Further optimization of the series resulted in the discovery of N-(biphenyl-3-ylmethyl)-2-(4-ethyl-6,6-dimethyl-2-oxomorpholin-3-yl)acetamide (87), which, in addition to fungicidal activity against Candida species, shows promising and broad antifungal in vitro activity against various fungi species, such as molds and dermatophytes. In vivo efficacy was also demonstrated in a murine model of systemic Candida albicans infection with a significant fungal load reduction in kidneys.
ANTIFUNGAL COMPOUNDS
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Page/Page column 66; 68, (2011/07/07)
The present invention relates to a series of novel compounds which have been shown to possess antifungal activity. The invention therefore relates to the new compounds, methods for their preparation, pharmaceutical compositions comprising them and to the compounds for use as a medicament, more in particular antifungal medicament.
