Peptidomimetics containing a vinyl ketone warhead as falcipain-2 inhibitors

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• 作者：Roberta Ettari ; Maria Zappalà ; Nicola Micale ; Giovanni Grazioso ; Salvatore Giofrè ; Tanja Schirmeister ; Silvana Grasso
• 关键词：Peptidomimetics ; Falcipain-2 inhibitors ; Cysteine proteases ; Docking studies
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2011
• 出版时间：June 2011
• 年：2011
• 卷：46
• 期：6
• 页码：2058-2065
• 全文大小：605 K

文摘

The design, chemical synthesis, and enzymatic activity evaluation of a set of falcipain-2 inhibitors are reported. These compounds contain a proven peptidomimetic recognition motif based on a benzo[1,4]diazepin-2-one (1,4-BDZ) framework built on a dipeptide sequence, and a Michael acceptor terminal moiety capable of deactivating the cysteine protease active site. Our goal is to modify the P₃ site of this motif in order to identify the structural requirements for the interaction with the target.