Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1370018 | Bioorganic & Medicinal Chemistry Letters | 2016 | 5 Pages |
Abstract
α-Keto amide derivatives as enterovirus 71 (EV71) 3C protease (3Cpro) inhibitors have been synthesized and assayed for their biochemical and antiviral activities. structure–activity relationship (SAR) study indicated that small moieties were primarily tolerated at P1′ and the introduction of para-fluoro benzyl at P2 notably improved the potency of inhibitor. Inhibitors 8v, 8w and 8x exhibited satisfactory activity (IC50 = 1.32 ± 0.26 μM, 1.88 ± 0.35 μM and 1.52 ± 0.31 μM, respectively) and favorable CC50 values (CC50 > 100 μM). α-Keto amide may represent a good choice as a warhead for EV71 3Cpro inhibitor.
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Related Topics
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Authors
Debin Zeng, Yuying Ma, Rui Zhang, Quandeng Nie, Zhengjie Cui, Yaxin Wang, Luqing Shang, Zheng Yin,