Design, synthesis, and antibacterial activity of novel myricetin derivatives containing sulfonate
Shijun Su, Qing Zhou, Xuemei Tang, Feng Peng, Tingting Liu, Liwei Liu, Chengwei Xie, Ming He, Wei Xue
Abstract
Abstract A series of myricetin derivatives containing sulfonate groups were designed and synthesized. Preliminary antibacterial activity showed that most of the target compounds exhibited significant biological activities against Xanthomonas axonopodis pv. Citri (Xac) , Ralstonia solanacearum (Rs) , and Xanthomonas oryzae pv. Oryzae (Xoo) . In particular, the EC 50 value of compound 3e was 13.76 μg/cm 3 against Xac , which was better than commercial reagents bismerthiazol (50.32 µg/cm 3 ) and thiodiazole copper. (83.27 µg/cm 3 ), and the EC 50 value of compound 3j was 11.92 μg/cm 3 against Xoo in vitro, The result was better than that of bismerthiazol (72.08 µg/cm 3 ) and thiodiazole copper (99.26 µg/cm 3 ). Compound 3j displayed the better in vivo activity against rice bacterial leaf blight than bismerthiazol and thiodiazole copper. Meanwhile, the antibacterial mechanism of compounds 3e and 3j was studied by scanning electron microscope (SEM). These results suggested that myricetin derivatives containing sulfonate can be considered as a new antibacterial reagents. Graphic abstract