Adamantane sulfone and sulfonamide 11-beta-HSD1 Inhibitors.
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.
Sorensen
Bryan
B
Abbott, Dept. 47F, Bldg. AP-10, Rm. 301, 100 Abbott Park Road, Abbott Park, IL 60064-6098, USA.
Winn
Martin
M
Rohde
Jeff
J
Shuai
Qi
Q
Wang
Jiahong
J
Fung
Steven
S
Monzon
Katina
K
Chiou
William
W
Stolarik
DeAnne
D
Imade
Hovis
H
Pan
Liping
L
Deng
Xiaoqing
X
Chovan
Linda
L
Longenecker
Kenton
K
Judge
Russell
R
Qin
Wenying
W
Brune
Michael
M
Camp
Heidi
H
Frevert
Ernst U
EU
Jacobson
Peer
P
Link
J T
JT
D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1 / Q000037:antagonists & inhibitors*; D043209:11-beta-Hydroxysteroid Dehydrogenase Type 2 / Q000037:antagonists & inhibitors; D000218:Adamantane / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology*; D000273:Adipose Tissue / Q000201:enzymology; D000818:Animals; D001921:Brain / Q000201:enzymology; D018360:Crystallography, X-Ray; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D006801:Humans; D007202:Indicators and Reagents; D008099:Liver / Q000201:enzymology; D051379:Mice; D008958:Models, Molecular; D013329:Structure-Activity Relationship
D004791:Enzyme Inhibitors; D007202:Indicators and Reagents; D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1; D043209:11-beta-Hydroxysteroid Dehydrogenase Type 2; D000218:Adamantane