Title of article
Adamantane 11-β-HSD-1 inhibitors: Application of an isocyanide multicomponent reaction
Author/Authors
Bryan Sorensen، نويسنده , , Jeff Rohde، نويسنده , , Jiahong Wang، نويسنده , , Steven Fung، نويسنده , , Katina Monzon، نويسنده , , William Chiou، نويسنده , , Liping Pan، نويسنده , , Xiaoqing Deng، نويسنده , , DeAnne Stolarik، نويسنده , , Ernst U. Frevert، نويسنده , , Peer Jacobson، نويسنده , , J.T Link، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
5
From page
5958
To page
5962
Abstract
A series of potent and selective adamantane aminoamide 11-β-HSD-1 inhibitors has been optimized. Chemically these studies were expedited by utilizing readily obtained amino acids as starting materials or an isocyanide multicomponent reaction. Structure–activity relationship studies resulted in the discovery of dual human and mouse 11-β-HSD-1 potent and selective inhibitors like adamantane 11and related compounds with high metabolic stability and robust pharmacokinetic profiles.
Keywords
HSD1 inhibitor , Hydroxysteroid dehydrogenase type 1 , 11-?-HSD-1 inhibitors , multicomponent reaction , metabolism , Adamantane , metabolic syndrome
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797507
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