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Synthesis and In-Vitro Evaluation of 2-Amino-4-arylthiazole As Inhibitor of 3D Polymerase Against Foot-and-mouth Disease (FMD)

European journal of medicinal chemistry(2015)

引用 28|浏览15
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摘要
Foot-and-mouth disease (FMD) is a highly contagious vesicular disease of livestock caused by a highly variable RNA virus, foot-and-mouth disease virus (FMDV). One of the targets to suppress expansion of and to control FMD is 3D polymerase (FMDV 3Dpol). In this study, 2-amino-4-arylthiazole derivatives were synthesized and evaluated for their inhibitory activity against FMDV 3Dpol. Among them, compound 20i exhibited the most potent functional inhibition (IC50 = 0.39 μM) of FMDV 3D polymerase and compound 24a (EC50 = 13.09 μM) showed more potent antiviral activity than ribavirin (EC50 = 1367 μM) and T1105 (EC50 = 347 μM) with IBRS-2 cells infected by the FMDV O/SKR/2010 strain.
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关键词
Foot-and-mouth disease virus (FMDV),Antiviral,Inhibitor,3D polymerase (3Dpol),2-Amino-4-arylthiazole
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