Discovery and biological evaluation of adamantyl amide 11beta-HSD1 inhibitors

Scott P. Webster,Peter Ward,Margaret Binnie,Eilidh Craigie,Kirsty M.M. McConnell,Karen Sooy,Andy Vinter,Jonathan R. Seckl,Brian R. Walker

Discovery and biological evaluation of adamantyl amide 11beta-HSD1 inhibitors

2007

Scott P. Webster
Peter Ward
Margaret Binnie
Eilidh Craigie
Kirsty M.M. McConnell
Karen Sooy
Andy Vinter
Jonathan R. Seckl
Brian R. Walker

A series of adamantyl amide 11beta-HSD1 inhibitors has been discovered and chemically modified. Selected compounds are selective for 11beta-HSD1 over 11beta-HSD2 and possess excellent cellular potency in human and murine 11beta-HSD1 assays. Good pharmacodynamic characteristics are observed in ex vivo assays.

Keywords:

Adamantane
Organic chemistry
Chemical synthesis
Stereochemistry
In vitro
Biochemistry
Carboxamide
Ex vivo
Structure–activity relationship
Amide
Chemistry
Enzyme inhibitor

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