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Synthesis and Antiviral Activity of N-Phenylbenzamide Derivatives a Novel Class of Enterovirus 71 Inhibitors

机译:N-苯基苯甲酰胺衍生物一类新型肠病毒71抑制剂的合成和抗病毒活性。

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摘要

A series of novel N-phenylbenzamide derivatives were synthesized and their anti-EV 71 activities were assayed in vitro. Among the compounds tested, 3-amino-N-(4-bromophenyl)-4-methoxybenzamide (>1e) was active against the EV 71 strains tested at low micromolar concentrations, with IC50 values ranging from 5.7 ± 0.8–12 ± 1.2 μM, and its cytotoxicity to Vero cells (TC50 = 620 ± 0.0 μM) was far lower than that of pirodavir (TC50 = 31 ± 2.2 μM). Based on these results, compound >1e is a promising lead compound for the development of anti-EV 71 drugs.
机译:合成了一系列新颖的N-苯基苯甲酰胺衍生物,并在体外测定了它们的抗EV 71活性。在测试的化合物中,3-氨基-N-(4-溴苯基)-4-甲氧基苯甲酰胺(> 1e )在低微摩尔浓度下对EV 71菌株具有活性,IC50值为5.7± 0.8–12±1.2μM,其对Vero细胞的细胞毒性(TC50 = 620±0.0μM)远低于吡罗那韦(TC50 = 31±2.2μM)。基于这些结果,化合物> 1e 是开发抗EV 71药物的有前途的先导化合物。

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