Triazolopyrimidine-2-sulfonamide belongs to a herbicide group called acetohydroxyacid synthase inhibitors. With the aim to discover new triazolopyrimidine sulfonanilide compounds with high herbicidal activity and faster degradation rate in soil, the methyl group of Flumetsulam (FS) was modified into a methoxy group to produce a new herbicidal compound, N-2,6-difluorophenyl-5-methoxy-1,2,4-triazolo[1,5-a]pyrimidine-2-sulfonamide (experimental code: Y6610). The enzymatic kinetic results indicated that compound Y6610 and FS have k_i values of 3.31 × 10⁻⁶ M and 3.60 × 10⁻⁷ M against Arabidopsis thaliana AHAS, respectively. The 10-fold lower enzyme-inhibiting activity of Y6610 was explained rationally by further computational simulations and binding free energy calculations. In addition, compound Y6610 was found to display the same level in vivo post-emergent herbicidal activity as FS against some broad-leaf weeds and good safety to rice, maize, and wheat at the dosages of 75–300 g ai/ha. Further determination of the half-lives in soil revealed that the half-life in soil of Y6610 is 3.9 days shorter than that of FS. The experimental results herein showed that compound Y6610 could be regarded as a new potential acetohydroxyacid synthase-inhibiting herbicide candidate for further study.

三唑并嘧啶-2-磺酰胺属于称为乙酰羟酸合酶抑制剂的除草剂基团。为了发现在土壤中具有高除草活性和更快降解速度的新三唑并嘧啶磺酰苯胺化合物，将Flumetsulam（FS）的甲基改性为甲氧基，以生产新的除草化合物N -2,6-6-二氟苯基-5。 -甲氧基-1，2，4-三唑并[1，5- a ]嘧啶-2-磺酰胺（实验代码：Y6610）。酶动力学结果表明，化合物Y6610和FS已经ķ_我值的3.31×10 ^-6  M和3.60×10 ^-7 中号对拟南芥AHAS分别。通过进一步的计算模拟和结合自由能计算，可以合理地解释Y6610的10倍较低的酶抑制活性。此外，发现化合物Y6610的发芽后体内除草活性与FS对某些阔叶杂草的杀草活性相同，并且在75–300 g ai / ha的剂量下对稻米，玉米和小麦具有良好的安全性。进一步测定土壤的半衰期表明，Y6610的土壤半衰期比FS短3.9天。本文的实验结果表明，化合物Y6610 可以被认为是一种新的潜在的抑制乙酰羟酸合酶的除草剂，有待进一步研究。