Adamantyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.
Adamantyl triazoles were identified as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1). They are active both in in vitro and in in vivo pharmacodynamic models. The synthesis and structure-activity relationships of these inhibitors are presented.
Olson
Steven
S
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. steven_olson@merck.com
Aster
Susan D
SD
Brown
Kai
K
Carbin
Linda
L
Graham
Donald W
DW
Hermanowski-Vosatka
Anne
A
LeGrand
Cheryl B
CB
Mundt
Steven S
SS
Robbins
Michael A
MA
Schaeffer
James M
JM
Slossberg
Llnon H
LH
Szymonifka
Michael J
MJ
Thieringer
Rolf
R
Wright
Samuel D
SD
Balkovec
James M
JM
D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1 / Q000037:antagonists & inhibitors*; D000218:Adamantane / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology; D000818:Animals; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D024821:Metabolic Syndrome / Q000188:drug therapy; D051379:Mice; D010599:Pharmacokinetics; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology
D004791:Enzyme Inhibitors; D014230:Triazoles; D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1; D000218:Adamantane