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

Abstract:

: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.

journal_name

Bioorg Med Chem Lett

authors

Webster SP,Ward P,Binnie M,Craigie E,McConnell KM,Sooy K,Vinter A,Seckl JR,Walker BR

doi

10.1016/j.bmcl.2007.02.057

subject

Has Abstract

pub_date

2007-05-15 00:00:00

pages

2838-43

issue

10

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(07)00254-5

journal_volume

17

pub_type

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