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Discovery of adamantane ethers as inhibitors of 11β-HSD-1: Synthesis and biological evaluation

Authors :
Patel, Jyoti R.
Shuai, Qi
Dinges, Jurgen
Winn, Marty
Pliushchev, Marina
Fung, Steven
Monzon, Katina
Chiou, William
Wang, Jiahong
Pan, Liping
Wagaw, Seble
Engstrom, Kenneth
Kerdesky, Francis A.
Longenecker, Kenton
Judge, Russell
Qin, Wenying
Imade, Hovis M.
Stolarik, DeAnne
Beno, David W.A.
Brune, Michael
Source :
Bioorganic & Medicinal Chemistry Letters. Feb2007, Vol. 17 Issue 3, p750-755. 6p.
Publication Year :
2007

Abstract

Abstract: A novel class of adamantane ethers 11β-hydroxysteroid hydrogenase type I inhibitors has been discovered. These compounds have excellent HSD-1 potency and selectivity against HSD-2. The structure–activity relationships, selectivity, metabolism, PK, ex vivo pharmacodynamic data, and an X-ray crystal structure of one of these inhibitors bound to h-HSD-1 are discussed. [Copyright &y& Elsevier]

Details

Language :
English
ISSN :
0960894X
Volume :
17
Issue :
3
Database :
Academic Search Index
Journal :
Bioorganic & Medicinal Chemistry Letters
Publication Type :
Academic Journal
Accession number :
23740368
Full Text :
https://doi.org/10.1016/j.bmcl.2006.10.074