title: Synthesis and antiviral activity of N-phenylbenzamide derivatives, a novel class of enterovirus 71 inhibitors.
abstract: 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.
authors.affiliation: Institute of Medicinal Biotechnology, Chinese Academy of Medical Science and Peking Union Medical College, Beijing 100050, China.
authors.forename: Xing-Yue
authors.initials: XY
authors.lastname: Ji
authors.forename: Hui-Qiang
authors.initials: HQ
authors.lastname: Wang
authors.forename: Lan-Hu
authors.initials: LH
authors.lastname: Hao
authors.forename: Wei-Ying
authors.initials: WY
authors.lastname: He
authors.forename: Rong-Mei
authors.initials: RM
authors.lastname: Gao
authors.forename: Yan-Ping
authors.initials: YP
authors.lastname: Li
authors.forename: Yu-Huan
authors.initials: YH
authors.lastname: Li
authors.forename: Jian-Dong
authors.initials: JD
authors.lastname: Jiang
authors.forename: Zhuo-Rong
authors.initials: ZR
authors.lastname: Li
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D001549:Benzamides / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D002522:Chlorocebus aethiops; D004353:Drug Evaluation, Preclinical; D004770:Enterovirus / Q000187:drug effects; D020128:Inhibitory Concentration 50; D010880:Piperidines / Q000494:pharmacology / Q000633:toxicity; D011724:Pyridazines / Q000494:pharmacology / Q000633:toxicity; D013329:Structure-Activity Relationship; D014709:Vero Cells
chemical_list: D000998:Antiviral Agents; D001549:Benzamides; D010880:Piperidines; D011724:Pyridazines; C074589:pirodavir