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Two important cytokines mediating inflammation are tumor necrosis factor alpha (TNFalpha) and IL-1beta, both of which require conversion to soluble forms by converting enzymes. The importance of TNFalpha-converting enzyme and IL-1beta-converting enzyme in the production of circulating TNFalpha and IL-1beta in response to systemic challenges has been(More)
A series of alpha-ketooxadiazole compounds was prepared and evaluated in vitro as potential inhibitors of human neutrophil elastase (HNE), proteinase-3 (PR-3), and porcine pancreatic elastase (PPE). Several compounds have been found to be very potent, fast, reversible, and selective inhibitors of HNE with Ki values below 100 pM. The highest kon value(More)
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