Design, synthesis and antibacterial activity of quinazolinone derivatives containing glycosides

Abstract

A series of novel quinazolinone derivatives containing glycosides were designed and synthesized. The biological activities test found that this series of compounds had good antibacterial activities. Among all target compounds, compounds 1 and 15 showed good antibacterial activity in vitro against Pseudomonas syringae pv. actinidiae (Psa), with an EC50 value of 48.7 mg/L, 45.6 mg/L, respectively, which better than thiodiazole copper (54.6 mg/L) and zinc thiazole (49.2 mg/L). Compounds 15 and 23 showed good in vitro antibacterial activity against Xanthomonas oryzae pv. oryzae (Xoo) at a concentration of 100 mg/L, with inhibition rates of 79.3% and 77.1%, respectively, which better than thiodiazole copper (71.8%). In addition, compound 15 can cause significant deformation of cell surface.