
IndraLab
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"Analogs of Ep-475 (2a), designed to explore the role played by the carboxylate in epoxysuccinate thiol protease inhibitors, have been synthesized and tested as inhibitors of papain and cathepsin B. Papain and cathepsin B are rapidly inactivated by carboxylates 2a and 6a, but are inactivated much more slowly by 2b-2f, 6c, and 6f, in which the carboxylate is absent or replaced by an amide, ester, or ketone."