A highly stereoselective intramolecular 1,3-dipolar cycloaddition reaction of azomethine ylides derived from 2-vinyloxybenzaldehydes proceeded smoothly to allow for a direct access to tricyclic hexahydrobenzofuro[3,2-b]pyrroles in good yields.
The design, synthesis, and biological evaluation of structurally novel N-cyanopyrazolidine and N-cyanohexahydropyridazine derivatives as cathepsin inhibitors are described. In vitro assay reveals that several compounds exhibit highly potent and selective profiles against cathepsins K or S.
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