Synthesis, structure, and biological activity of novel (oxdi/tri)azoles derivatives containing 1,2,3-thiadiazole or methyl moiety

To develop novel inhibitors of ketol-acid reductoisomerase, a series of (oxdi/tri)azoles derivatives was synthesized and characterized by (1)H NMR, MS, elemental analyses, and crystallography. According to the biological activities of these compounds obtained both in vivo and in vitro, compound 4-cyclopropyl-3-((4-fluorobenzyl)thio)-5-methyl-4H-1,2,4-triazole showed excellent KARI inhibitory activity (100% at 100?μg?mL?(-1) in vitro). In addition, most of the title compounds exhibited good herbicidal activity against Brassica campestris in vivo.