Bicyclic carbamates as inhibitors of papain-like cathepsin proteases

…, H Liu, D Mason, B Bursulaya, C Tumanut, J Li…

文献索引：Epple, Robert; Urbina, Hugo D.; Russo, Ross; Liu, Hong; Mason, Daniel; Bursulaya, Badry; Tumanut, Christine; Li, Jun; Harris, Jennifer L. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 5 p. 1254 - 1259

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被引用次数: 7

摘要

A 6-oxa-1-aza-bicyclo [3.2. 1] octan-7-one system inhibits the proteolytic activity of several cysteine proteases belonging to the papain family. In vitro mechanistic studies and in silico calculations suggest that the minimal π-overlap between the bridgehead nitrogen and the carbonyl leads to a considerable weakening of the urethane system, making it susceptible to nucleophilic attack from the active site thiol group. The resulting covalent adduct is slowly ...