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 activit...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.展开更多
基金supported by the National Natural Science Foundation of China(Nos.21362004,21562013)Subsidy Project for Outstanding Key Laboratory of Guizhou Province in China(20154004)
文摘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.