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  • Sulfonamide derivatives of bridgehead substituted bicyclo[4.2.1]nonanes as gamma-secretase inhibitors.

Sulfonamide derivatives of bridgehead substituted bicyclo[4.2.1]nonanes as gamma-secretase inhibitors.

Bioorganic & medicinal chemistry letters (2007-12-07)
Tim Sparey, Earl Clarke, Joanne Hannam, Timothy Harrison, Andrew Madin, Mark Shearman, Bindi Sohal
PMID18061448
ABSTRACT

Bridgehead substituted derivatives of bicyclo[4.2.1]nonanes were synthesized and shown to be potent inhibitors of gamma-secretase. Two related series were synthesized to explore the SARs. More potent compounds were found in the non-benzofused series compared with the benzofused series. One compound from each series showed good exposure in the hepatic portal vein (HPV) following oral dosing to rats.