N-Substituted pyrazole-3-carboxamides as inhibitors of human 15-lipoxygenase

[Display omitted] High-throughput screening was used to find selective inhibitors of human 15-lipoxygenase-1 (15-LOX-1). One hit, a 1-benzoyl substituted pyrazole-3-carboxanilide (1a), was used as a starting point in a program to develop potent and selective 15-LOX-1 inhibitors.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2015-08, Vol.25 (15), p.3017-3023
Hauptverfasser:	Pelcman, Benjamin, Sanin, Andrei, Nilsson, Peter, Schaal, Wesley, Olofsson, Kristofer, Krog-Jensen, Christian, Forsell, Pontus, Hallberg, Anders, Larhed, Mats, Boesen, Thomas, Kromann, Hasse, Claesson, Hans-Erik
Format:	Artikel
Sprache:	eng
Schlagworte:	15-Lipoxygenase Amides - chemistry Amides - pharmacology Arachidonate 15-Lipoxygenase - metabolism Arachidonic acid Humans Inhibitors Lipoxygenase Inhibitors - chemistry Lipoxygenase Inhibitors - pharmacology Pyrazole Pyrazoles - chemistry Pyrazoles - pharmacology
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Beschreibung
Zusammenfassung:	[Display omitted] High-throughput screening was used to find selective inhibitors of human 15-lipoxygenase-1 (15-LOX-1). One hit, a 1-benzoyl substituted pyrazole-3-carboxanilide (1a), was used as a starting point in a program to develop potent and selective 15-LOX-1 inhibitors.
ISSN:	0960-894X 1464-3405 1464-3405
DOI:	10.1016/j.bmcl.2015.05.007