Synthesis and Bioactivities of Novel 1,3,4-Thiadiazole Derivatives of Glucosides

Abstract

A series of novel 1,3,4-thiadiazole derivatives of glucosides were synthesized by the starting materials <i>d</i>-glucose and 5-amino-1,3,4-thiadiazole-2-thiol in good yields with employing a convergent synthetic route. The results of bioactivities showed that some of the target compounds exhibited good antifungal activities. Especially, compounds <b>4i</b> showed higher bioactivities against <i>Phytophthora infestans</i> (<i>P. infestans</i>), with the EC₅₀ values of 3.43, than that of Dimethomorph (5.52 μg/ml). In addition, the target compounds exhibited moderate to poor antibacterial activities against <i>Xanthomonas oryzae p</i>v. <i>oryzae</i> (<i>Xoo</i>)<i>, Xanthomonas campestris p</i>v. <i>citri</i> (<i>Xcc</i>).