Adamantane 11-β-HSD-1 inhibitors: Application of an isocyanide multicomponent reaction
Copyright policy )Adamantane 11-β-HSD-1 inhibitors: Application of an isocyanide multicomponent reaction
A series of potent and selective adamantane aminoamide 11-beta-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-beta-HSD-1 potent and selective inhibitors like adamantane 11 and related compounds with high metabolic stability and robust pharmacokinetic profiles.
Cyanides, Molecular Structure, Adamantane, Mice, Structure-Activity Relationship, 11-beta-Hydroxysteroid Dehydrogenase Type 2, 11-beta-Hydroxysteroid Dehydrogenase Type 1, Animals, Humans, Enzyme Inhibitors
Cyanides, Molecular Structure, Adamantane, Mice, Structure-Activity Relationship, 11-beta-Hydroxysteroid Dehydrogenase Type 2, 11-beta-Hydroxysteroid Dehydrogenase Type 1, Animals, Humans, Enzyme Inhibitors
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