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乙酰羟基酸合成酶(Acetohydroxyacid synthase,AHAS,EC4.1.3.18)是植物和微生物中亮氨酸、异亮氨酸和缬氨酸合成途径的一个关键酶,以AHAS为靶标的磺酰脲类除草剂具有高效、高选择性和对环境友好的特点.通过2-氨基-4-甲基嘧啶溴代反应以及进一步的衍生、磺酰基异氰酸酯的胺解,合成了一系列含有5-溴嘧啶基的新磺酰脲.其结构经1HNMR、质谱和元素分析确定.生物活性测试表明目标化合物在离体水平对大肠杆菌乙酰羟基酸合成酶同工酶AHASII表现出了与市售除草剂苯磺隆相当甚至更优的抑制活性,而盆栽除草活性低于苯磺隆.
Acetohydroxyacid synthase (AHAS, EC 4.1.3.18) is a key enzyme involved in the synthesis of leucine, isoleucine and valine in plants and microorganisms, sulfonylureas targeting AHAS Herbicides have the characteristics of high efficiency, high selectivity and environmental friendliness.A series of 5-bromopyrimidinyl (5-bromopyrimidinyl) -pyrimidine derivatives were synthesized by the bromination of 2-amino-4-methylpyrimidine and further derivatisation of sulfonyl isocyanate Of the new sulfonylurea.The structure was confirmed by 1HNMR, mass spectrometry and elemental analysis.The biological activity test showed that the target compound exhibited high activity against E.coli acetohydroxy acid synthase isozyme AHASII at the exogenous level with the herbicide tribenuron-methyl Quite even better inhibitory activity, while the potting herbicidal activity is lower than that of tribenuron-methyl.