Design, synthesis and antibacterial activity of quinazolinone derivatives containing glycosides

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 <b>1</b> and <b>15</b> showed good antibacterial activity <i>in vitro</i> against <i>Pseudomonas syringae</i> pv. <i>actinidiae</i> (<i>Psa</i>), 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 <b>15</b> and <b>23</b> showed good <i>in vitro</i> antibacterial activity against <i>Xanthomonas oryzae</i> pv. <i>oryzae</i> (<i>Xoo</i>) 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 <b>15</b> can cause significant deformation of cell surface.