Examination of peptidic α′,β-diamino-α,α-difluoroketones as inhibitors of human leukocyte elastase

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Abstract

The preparation and in vitro evaluation of a series of peptidic α′,β-diamino-α,α-difluoroketones are described. Comparison of the efficacy of these compounds to both their corresponding trifluoromethylketone and α-carboxamido-α,α-difluoroketone inhibitors reveals a divergent set of structure-activity relationships. This divergence indicates that the inhibitor's P1′-amino group is strongly interacting with the enzyme's S1′-subsite.

The preparation and in vitro evaluation of a series of peptidic α′,β-diamino-α,α-difluoroketones are described. Comparison of the efficacy of these compounds to both their corresponding trifluoromethylketone and α-carboxamido-α,α-difluoroketone inhibitors reveals a divergent set of structure-activity relationships. This divergence indicates that the inhibitor's P1′-amino group is strongly interacting with the enzyme's S1′-subsite.

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