Design, synthesis, and in vivo activity of novel inhibitors of delta-5 desaturase for the treatment of metabolic syndrome

[Display omitted] The synthesis, SAR, and in vivo activity of inhibitors of delta-5 desaturase are described. Ring-constraint of the initial series provided access to a variety of in vitro active chemotypes, from which the indazole was selected. Examples from the indazole series displayed in vivo ac...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2015-09, Vol.25 (18), p.3836-3839
Hauptverfasser:	Baugh, Simon D.P., Pabba, Praveen K., Barbosa, Joseph, Coulter, Eric, Desai, Urvi, Gay, Jason P., Gopinathan, Suma, Han, Qiang, Hari, Rajee, Kimball, S. David, Nguyen, Huy V., Ni, Chi-You, Powell, David R., Smith, Arian, Terranova, Kristen M., Wilson, Alan, Yu, Xuan-Chuan, Lombardo, Victoria K.
Format:	Artikel
Sprache:	eng
Schlagworte:	Amides - chemical synthesis Amides - chemistry Amides - pharmacology Animals Delta-5 desaturase Dose-Response Relationship, Drug Drug Design Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Fatty Acid Desaturases - antagonists & inhibitors Fatty Acid Desaturases - metabolism Humans In vivo efficacy Indazole Liver - enzymology Metabolic syndrome Metabolic Syndrome - drug therapy Metabolic Syndrome - enzymology Metabolic Syndrome - metabolism Mice Molecular Structure Ring constraint Structure-Activity Relationship
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Zusammenfassung:	[Display omitted] The synthesis, SAR, and in vivo activity of inhibitors of delta-5 desaturase are described. Ring-constraint of the initial series provided access to a variety of in vitro active chemotypes, from which the indazole was selected. Examples from the indazole series displayed in vivo activity in reducing the enzymatic activity of liver delta-5 desaturase.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2015.07.066