Design, synthesis, and evaluation of a novel series of macrocyclic inhibitors of norovirus 3CL protease

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• 作者：Vishnu C. Damalanka^a ; Yunjeong Kim^b ; Anushka C. Galasiti Kankanamalage^a ; Gerald H. Lushington^c ; Nurjahan Mehzabeen^d ; Kevin P. Battaile^e ; Scott Lovell^d ; Kyeong-Ok Chang^b ; ^{kchang@vet.ksu.edu} ; William C. Groutas^a ; ^{bill.groutas@wichita.edu}
• 关键词：Macrocyclic inhibitors ; Norovirus ; 3CLprotease
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：127
• 期：Complete
• 页码：41-61
• 全文大小：3068 K
• 卷排序：127

文摘

A novel series of macrocyclic inhibitors of norovirus 3CL protease inhibitors is reported. High resolution crystal structures of enzyme-inhibitor complexes have confirmed the mechanism of action. The structural determinants involved in binding have been delineated. The inhibitor design rationale was validated by x-ray crystallographic studies.