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Azabicyclic sulfonamides as potent 11beta-HSD1 inhibitors.

Abstract：

:Inhibition of 11beta-HSD1 has demonstrated potential in the treatment of various components of metabolic syndrome. We wish to report herein the discovery of novel azabicyclic sulfonamide based 11beta-HSD1 inhibitors. Highly potent compounds exhibiting inhibitory activities at both human and mouse 11beta-HSD1 were identified. Several compounds demonstrated significant in vivo activity in the mouse cortisone challenge assay.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Shah U,Boyle CD,Chackalamannil S,Baker H,Kowalski T,Lee J,Terracina G,Zhang L

doi

10.1016/j.bmcl.2010.01.082

subject

Has Abstract

pub_date

2010-03-01 00:00:00

pages

1551-4

issue

5

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(10)00094-6

journal_volume

20

pub_type

杂志文章

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