Study of the synthesis, antiviral bioactivity and interaction mechanisms of novel chalcone derivativ

来源 :Chinese Chemical Letters | 被引量 : 0次 | 上传用户:liupingxiu
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A series of novel chalcone derivatives that contain the 1,1-dichloropropene moiety was designed and synthesized. Bioactivity assays showed that most of the target compounds exhibited moderate to good antiviral activity against tobacco mosaic virus(TMV) at 500 mg/m L. Among the target compounds,compound 7h showed the highest in vivo inactivation activity against TMV with the EC50 and EC90value of 45.6 and 327.5 mg/m L, respectively, which was similar to that of Ningnanmycin(46.9 and 329.4 mg/m L)and superior to that of Ribavirin(145.1 and 793.1 mg/m L). Meanwhile, the microscale thermophoresis and fluorescence spectroscopy experiments showed that the compound 7h had a strong interaction with the tobacco mosaic virus coat protein. A series of novel chalcone derivatives that contain the 1,1-dichloropropene moiety was designed and synthesized. Bioactivity assays showed that most of the target compounds exhibited moderate to good antiviral activity against tobacco mosaic virus (TMV) at 500 mg / m L. Among the target compounds, compound 7h showed the highest in vivo inactivation activity against TMV with the EC50 and EC90 value of 45.6 and 327.5 mg / m L, respectively, which were similar to that of Ningnanmycin (46.9 and 329.4 mg / m L) and superior to that of Ribavirin (145.1 and 793.1 mg / mL). Meanwhile, the microscale thermophoresis and fluorescence spectroscopy experiments showed that the compound 7h had a strong interaction with the tobacco mosaic virus coat protein.
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