1184944-63-5Relevant academic research and scientific papers
Synthesis and Broad Antiviral Activity of Novel 2-aryl-isoindolin-1-ones towards Diverse Enterovirus A71 Clinical Isolates
Wang, Yixuan,Wang, Huiqiang,Jiang, Xinbei,Jiang, Zhi,Guo, Tingting,Ji, Xingyue,Li, Yanping,Li, Yuhuan,Li, Zhuorong
, (2019)
Enterovirus 71 (EV-A71) is the main causative pathogen of childhood hand, foot and mouth disease. Effective medicine is currently unavailable for the treatment of this viral disease. Using the fragment-hopping strategy, a series of 2-aryl-isoindolin-1-one compounds were designed, synthesized and investigated for their in vitro antiviral activity towards multiple EV-A71 clinical isolates (H, BrCr, Shenzhen98, Jiangsu52) in Vero cell culture in this study. The structure–activity relationship (SAR) studies identified 2-phenyl-isoindolin-1-ones as a new potent chemotype with potent antiviral activity against EV-A71. Ten out of the 24 tested compounds showed significant antiviral activity (EC50 50) values in the range of 1.23–1.76 μM. Moreover, the selectivity indices of A3 and A4 were significantly higher than those of the reference compound, pirodavir. The western blotting experiment indicated that the viral VP1 was significantly decreased at both the protein and RNA level in a dose-dependent manner following treatment with compound A3. Moreover, compound A3 inhibited the viral replication by acting on the virus entry stage. In summary, this study led to the discovery of 2-aryl-isoindolin-1-ones as a promising scaffold with potent anti-EV-A71 activities, which deserves further in-depth studies.
AROMATIC AMIDE DERIVATIVE
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Page/Page column 7, (2011/04/18)
A compound represented by the following general formula (I) (R1 and R2 represent hydrogen atom, an alkyl group, a halogen atom, etc.; R3 and R4 represent hydrogen atom, an alkyl group, an alkoxy group, or an alk
