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对羟苯基丙酮酸双氧化酶(EC 1.13.11.27,HPPD)是一个重要的除草剂作用靶标.为了寻找具有高效除草活性的新型HPPD抑制剂,在前期研究的基础上设计合成了24个含有喹唑啉二酮结构的三酮类化合物9a~9x.所合成的化合物均经过1H NMR,13C NMR和HRMS的表征.以来源于拟南芥的HPPD(At HPPD)为测试对象进行酶抑制活性筛选,结果表明所合成的大部分化合物对At HPPD均表现出了较好的抑制效果,其中化合物9i的Ki值为0.005μmol/L,显著优于商品化对照药剂硝磺草酮(Ki=0.013μmol/L).进一步温室盆栽筛选结果表明,多数化合物在150 g ai/ha的剂量下对六种供试杂草中的至少一种表现出80%以上的防效,特别是化合物9g在37.5 g ai/ha的低剂量下对所测试的六种杂草中的四种仍表现出了大于85%的抑制效果,同时9g在150 g ai/ha的剂量下对水稻和小麦均表现出了很好的作物安全性,可以作为先导化合物供进一步深入研究.
P-hydroxyphenylpyruvate dioxygenase (EC 1.13.11.27, HPPD) is an important herbicide target.In order to find a new type of HPPD inhibitor with high herbicidal activity, based on the previous study, we designed and synthesized 24 Quinazoline dione structure of the triketones 9a ~ 9x. The synthesized compounds were characterized by 1H NMR, 13C NMR and HRMS. To HPPD (At HPPD) derived from Arabidopsis for the test object enzyme inhibition activity The results showed that most of the compounds synthesized showed good inhibitory activity against At HPPD. The Ki value of compound 9i was 0.005 μmol / L, which was significantly better than that of the commercial comparator mesotrione (Ki = 0.013 μmol / L) .Further greenhouse pot screening showed that most compounds exhibited over 80% control efficacy against at least one of the six tested weeds at a dose of 150 g ai / ha, especially at a dose of 37.5 Four of the six tested weeds still exhibited greater than 85% inhibition at low doses of g ai / ha, while 9g showed rice and wheat at 150 g ai / ha Good crop safety can be used as a lead compound for further depth the study.