Design, Synthesis, and Antiviral Activity of Novel Chalcone Derivatives Containing a Purine Moiety

To find new antiviral agents, novel chalcone derivatives containing a purine moiety were designed and synthesized by combining bioactive substructures. The antiviral activities of the derivatives against tobacco mosaic virus ( TMV ) and cucumber mosaic virus ( CMV ) were evaluated. Results showed that most of the derivatives showed antiviral activities. Compounds 3n and 3p exhibited excellent curative, protective and inactivation activities against TMV , with the EC 50 values of 452.4, 416.2, 241.2 and 438.7, 418.6, 261.7 µg• mL −1 , respectively, which were better than those of ribavirin (585.8, 436.0 and 268.7 µg• mL −1 ). Compounds 3n and 3p showed remarkable curative and protective activities against CMV . Compound 3n showed a moderate affinity to TMV coat protein, with binding constant K a and K d values of 1.5 × 10 4 L•mol −1 and 79.8 µmol•L −1 , respectively. These findings provided an important structural insight for further designs of highly active chalcone derivatives and a basis for further study on their mechanism of action.