Design, Synthesis and Biological Activity of Ethyl 2-(N-Substituted-arylsulfonamido)-2-oxoacetate

Thirteen new ethyl 2-(N-substituted-arylsulfonamido)-2-oxoacetate(3a-3m), based on the structure of Ketol-acid reductoisomerase(KARI) inhibitor IpOHA, were designed and synthesized. Their structures were established on the basis of 1H NMR, IR, MS, and elemental analyses. The bioassay result reveals that the structural changes from hydroxyl group on the N atom of IpOHA to arylsulfonyl groups does not enhance the inhibitory activity of the compounds to KARI in vitro. Compounds 3c, 3h, 3k, and 3m are more effective than IpOHA against the monocotyledonous barnygrass at 100 μg/mL in herbicidal tests.