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
A series of novel chalcone derivatives containing purine moiety was designed and synthesized, and their antiviral activities against cucumber mosaic virus （CMV） and tobacco mosaic virus （TMV） were evaluated in viv...A series of novel chalcone derivatives containing purine moiety was designed and synthesized, and their antiviral activities against cucumber mosaic virus （CMV） and tobacco mosaic virus （TMV） were evaluated in vivo. Bioactivity assays indicated that some compounds showed good antiviral activities against CMV and TMV. It is worth mentioning that compounds 30, 3s, 3w, and 3x exhibited excellent curative activity against CMV, with ECso values of 301.1 μg/mL, 315.7 μg/mL, 282.3 μg/mL, 230.5 μg/mL, respectively, which were better than that of Dufulin （373.7 μg/mL） and Ribavirin （726.3 μg/mL）. In addition, the fluorescence spectroscopy experiment results showed that compound 3o showed strong combining capacity to tobacco mosaic virus coat orotein.展开更多
A new one-step synthesis of 3-hydroxymethylbenzofuran, based on intramolecular cyclization of 2- （methoxymethyl）-2-（2＇-methoxymethyl-4＇-methylphenyl）-butanone I under diluted hydrochloric acid in THF, was develo...A new one-step synthesis of 3-hydroxymethylbenzofuran, based on intramolecular cyclization of 2- （methoxymethyl）-2-（2＇-methoxymethyl-4＇-methylphenyl）-butanone I under diluted hydrochloric acid in THF, was developed. The mechanism for this process was investigated via chemical equilibrium shift of tautomer in acidic conditions. The applicability of this new method was studied further in this paper.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.
基金supported by the National Natural Science Foundation of China(Nos. 21562013 and 21362004)Subsidy Project for Outstanding Key Laboratory of Guizhou Province in China(No. 20154004)+1 种基金the Provincial University Cooperation Plan of Guizhou Province in China(No. 20147001)Collaborative Innovation Center for Natural Products and Biological Drugs of Yunnan
文摘A series of novel chalcone derivatives containing purine moiety was designed and synthesized, and their antiviral activities against cucumber mosaic virus （CMV） and tobacco mosaic virus （TMV） were evaluated in vivo. Bioactivity assays indicated that some compounds showed good antiviral activities against CMV and TMV. It is worth mentioning that compounds 30, 3s, 3w, and 3x exhibited excellent curative activity against CMV, with ECso values of 301.1 μg/mL, 315.7 μg/mL, 282.3 μg/mL, 230.5 μg/mL, respectively, which were better than that of Dufulin （373.7 μg/mL） and Ribavirin （726.3 μg/mL）. In addition, the fluorescence spectroscopy experiment results showed that compound 3o showed strong combining capacity to tobacco mosaic virus coat orotein.
基金supported by the National Mega-Project for Innovative Drugs (No. 2012zx09301002-002)State Key Laboratory of Bioactive Substance and Function of Natural Medicines
文摘A new one-step synthesis of 3-hydroxymethylbenzofuran, based on intramolecular cyclization of 2- （methoxymethyl）-2-（2＇-methoxymethyl-4＇-methylphenyl）-butanone I under diluted hydrochloric acid in THF, was developed. The mechanism for this process was investigated via chemical equilibrium shift of tautomer in acidic conditions. The applicability of this new method was studied further in this paper.
