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ID: ALA1145299
Journal: Bioorg Med Chem Lett
Title: Adamantane 11-beta-HSD-1 inhibitors: Application of an isocyanide multicomponent reaction.
Authors: Sorensen B, Rohde J, Wang J, Fung S, Monzon K, Chiou W, Pan L, Deng X, Stolarik D, Frevert EU, Jacobson P, Link JT.
Abstract: 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.
CiteXplore: 16996734