Discovery of orally active butyrolactam 11β-HSD1 inhibitors

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

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2006-11, Vol.16 (21), p.5555-5560
Hauptverfasser:	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:	Artikel
Sprache:	eng
Schlagworte:	11b-HSD1 inhibitors Biological and medical sciences Butyrolactams General and cellular metabolism. Vitamins Medical sciences Pharmacodynamic Pharmacokinetic Pharmacology. Drug treatments
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Beschreibung
Zusammenfassung:	A series of metabolically stable butyrolactam 11β-HSD1 inhibitors have been synthesized and biologically evaluated. A series of metabolically stable butyrolactam 11β-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
DOI:	10.1016/j.bmcl.2006.08.034