Design, Synthesis And Biological Activity Studies Of Chalcone Derivatives Containing Hydrazine

Purine derivatives,which have widely biological activities,are introduced into chalcone compounds,a series of novel chalcone derivatives containing purine group 3a-3z were designed and synthesized.The antiviral activities of the target compounds was measuremented by half-leaf spot method,cucumber mosaic virus and tobacco mosaic virus as research object,meanwhile the interaction between TMV CP and target compounds was preliminarily studied.The main conclusions of this paper are summarized as follows:1.In order to find new antiviral candidate drugs,novel chalcone derivatives containing purine group were designed and synthesized based on the principle of combinating bioactive substructures.The physical characteristics were confirmed by 1H NMR,13 C NMR,IR and HRMS.2.At the concentration of 500 ?g/mL,the antiviral activities of the target compounds against CMV and TMV in vivo were tested in accordance with the reported method.The results showed that most of the compounds showed good curative activities against CMV.Based on the findings,the EC50 values of curative activities against CMV of all the compounds were tested.The data indicated that compounds 3o,3s,3w,and 3x displayed excellent curative effects against CMV with EC50 values of 301.1,315.7,282.3,and 230.5 ?g/m L,respectively,which were better than that of Ningnanmycin(EC50 = 343.8 ?g/m L)and Ribavirin(EC50 = 726.3 ?g/m L);In the antiTMV activity,the inactivating activities of compounds 3o and 3p were 89.1% and 88.2%,respectively,which were comparable to that of Ningnanmycin(89.5%).3.The interaction between the compound 3o with TMV CP was further investigated by fluorescence spectroscopy.The results showed that there were interaction between compound 3o and TMV CP.