Discovery of orally active butyrolactam 11β-HSD1 inhibitors

Vince Yeh,Ravi Kurukulasuriya,Steven Fung,Katina Monzon,William Chiou,Jiahong Wang,DeAnne Stolarik,Hovis M. Imade,Robin Shapiro,Victoria Knourek-Segel,Eugene N. Bush,Denise Wilcox,Phong Nguyen,Michael E. Brune,Peer B. Jacobson,J. T. Link

Discovery of orally active butyrolactam 11β-HSD1 inhibitors

2006

Vince Yeh
Ravi Kurukulasuriya
Steven Fung
Katina Monzon
William Chiou
Jiahong Wang
DeAnne Stolarik
Hovis M. Imade
Robin Shapiro
Victoria Knourek-Segel
Eugene N. Bush
Denise Wilcox
Phong Nguyen
Michael E. Brune
Peer B. Jacobson
J. T. Link

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.

Keywords:

Organic chemistry
Enzyme
Pharmacodynamics
Potency
Biochemistry
Chemistry
Enzyme inhibitor
Pharmacokinetics
Selectivity
Chemical synthesis
Oral administration
Lactam
In vivo
Stereochemistry

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