Synthesis and antifungal and antibacterial evaluation of novel pyrimidine derivatives with glycoside scaffolds

In order to discover new leading compounds with high antifungal and antibacterial activities, in this study, fifteen novel pyrimidine derivatives with glycoside scaffolds were synthesized using d-glucose as a starting material by five-step reactions. All of the newly synthesized compounds were screened for their in vitro antifungal activities against Phytophthora infestans, Gibberella zeae, Botryosphaeria dothidea, Phompsis sp., Thanatephorus cucumeris, and antibacterial activities against Xanthomonas oryzae pv. oryzae and Xanthomonas citri subsp. citri. Bioassay results indicated that compounds 4l, 4m, and 4o showed better in vitro antifungal activity against P. infestans, with the EC50 values of 3.42, 3.99, and 2.73 μg/mL, respectively, than that of dimethomorph (4.49 μg/mL).