Discovery of orally active butyrolactam 11beta-HSD1 inhibitors

A series of metabolically stable butyrolactam 11beta-HSD1 inhibitors have been synthesized and biologically evaluated. These compounds exhibit excellent HSD1 potency and HSD2 selectivity, pharmacokinetic, and pharmacodynamic profiles.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2006-11, Vol.16 (21), p.5555-5560
Main Authors: Yeh, Vince S C, Kurukulasuriya, Ravi, Fung, Steven, Monzon, Katina, Chiou, William, Wang, Jiahong, Stolarik, Deanne, Imade, Hovis, Shapiro, Robin, Knourek-Segel, Victoria, Bush, Eugene, Wilcox, Denise, Nguyen, Phong T, Brune, Michael, Jacobson, Peer, Link, J T
Format: Article
Language:English
Subjects:
11-beta-Hydroxysteroid Dehydrogenase Type 1 - antagonists & inhibitors
Administration, Oral
Animals
Humans
Lactams - administration & dosage
Lactams - chemical synthesis
Lactams - pharmacokinetics
Lactams - pharmacology
Metabolic Syndrome - drug therapy
Mice
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Description
Summary:A series of metabolically stable butyrolactam 11beta-HSD1 inhibitors have been synthesized and biologically evaluated. These compounds exhibit excellent HSD1 potency and HSD2 selectivity, pharmacokinetic, and pharmacodynamic profiles.
ISSN:0960-894X
1464-3405