Discovery of potent and selective inhibitors of 11beta-HSD1 for the treatment of metabolic syndrome

High throughput screening efforts have identified a novel class of dichloroaniline amide 11beta-HSD1 inhibitors. SAR studies initiated from dichloroaniline 4 focused on retaining the potency and selectivity profile of the lead.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2006-12, Vol.16 (24), p.6241-6245
Hauptverfasser:	Richards, Steven, Sorensen, Bryan, Jae, Hwan-Soo, Winn, Marty, Chen, Yixian, Wang, Jiahong, Fung, Steven, Monzon, Katina, Frevert, Ernst U, Jacobson, Peer, Sham, Hing, Link, J T
Format:	Artikel
Sprache:	eng
Schlagworte:	11-beta-Hydroxysteroid Dehydrogenase Type 1 - antagonists & inhibitors Carbenoxolone - chemistry Carbenoxolone - pharmacology Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology Enzyme Inhibitors - therapeutic use Humans Metabolic Syndrome - drug therapy Molecular Conformation Piperazines - chemistry Piperazines - pharmacology Sulfonamides - chemistry Sulfonamides - pharmacology Thiazoles - chemistry Thiazoles - pharmacology
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Beschreibung
Zusammenfassung:	High throughput screening efforts have identified a novel class of dichloroaniline amide 11beta-HSD1 inhibitors. SAR studies initiated from dichloroaniline 4 focused on retaining the potency and selectivity profile of the lead.
ISSN:	0960-894X