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 ,
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
