Identification of fused bicyclic derivatives of pyrrolidine and imidazolidinone as dengue virus-2 NS2B-NS3 protease inhibitors

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• 作者：Zhibing Weng^a ; ¹ ; Xiaoxia Shao^b ; ¹ ; Dominik Graf^c ; Chunguang Wang^b ; Christian D. Klein^c ; Jing Wang^d ; ^{wangjing@njau.edu.cn} ; Guo-Chun Zhou^a ; ^{gczhou@njtech.edu.cn}
• 关键词：Dengue virus NS2B-NS3 protease inhibitor ; pyrrolidino[1 ; 2-c]imidazolidinone ; Stereochemistry ; Substitution and substituent ; Linker ; Structure-activity relationship (SAR)
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：5 January 2017
• 年：2017
• 卷：125
• 期：Complete
• 页码：751-759
• 全文大小：1185 K
• 卷排序：125

文摘

Fused compounds of pyrrole and imidazole were synthesized and studied against NS2B-NS3 protease. Fused compound 2 and linear compound 1 show activity against DENV-2 virus and NS2B-NS3 protease. Substituent and its stereochemistry at C-3 position are important for the inhibitory activity. Both of substitution (X) and a linker (Y) affect the inhibitory activity.