Adamantane sulfone and sulfonamide 11-beta-HSD1 Inhibitors

Bryan Sorensen; Martin Winn; Jeff Rohde; Qi Shuai; Jiahong Wang; Steven Fung; Katina Monzon; William Chiou; DeAnne Stolarik; Hovis Imade; Liping Pan; Xiaoqing Deng; Linda Chovan; Kenton Longenecker; Russell Judge; Wenying Qin; Michael Brune; Heidi Camp; Ernst U Frevert; Peer Jacobson; J T Link

doi:10.1016/j.bmcl.2006.10.008

Adamantane sulfone and sulfonamide 11-beta-HSD1 Inhibitors

Bioorg Med Chem Lett. 2007 Jan 15;17(2):527-32. doi: 10.1016/j.bmcl.2006.10.008. Epub 2006 Oct 7.

Affiliation

¹ Abbott, Dept. 47F, Bldg. AP-10, Rm. 301, 100 Abbott Park Road, Abbott Park, IL 60064-6098, USA.

PMID: 17070044
DOI: 10.1016/j.bmcl.2006.10.008

Abstract

Potent and selective adamantane sulfone and sulfonamide inhibitors of 11-beta-HSD-1 have been discovered. Selected compounds from these series have robust pharmacokinetic profiles and strongly inhibit liver, fat, and brain HSD1 for extended periods after oral dosing.

MeSH terms

11-beta-Hydroxysteroid Dehydrogenase Type 1 / antagonists & inhibitors*
11-beta-Hydroxysteroid Dehydrogenase Type 2 / antagonists & inhibitors
Adamantane / analogs & derivatives*
Adamantane / chemical synthesis*
Adamantane / pharmacology*
Adipose Tissue / enzymology
Animals
Brain / enzymology
Crystallography, X-Ray
Drug Design
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / pharmacokinetics
Enzyme Inhibitors / pharmacology*
Humans
Indicators and Reagents
Liver / enzymology
Mice
Models, Molecular
Structure-Activity Relationship

Substances

Enzyme Inhibitors
Indicators and Reagents
11-beta-Hydroxysteroid Dehydrogenase Type 1
11-beta-Hydroxysteroid Dehydrogenase Type 2
Adamantane