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为了发现高效、低毒、低残留的农药先导化合物,模拟AdSS酶天然抑制剂的活性结构,以L-酪氨酸为起始原料,经过关环和酯化等反应合成了24个新的5-(4-羟基苄基)-2,4-咪唑啉二酮酯系列化合物6a～6x,它们的结构通过IR,~1HNMR和元素分析进行了确证.化合物6m经X射线衍射测定:C_(18)H_(16)N_2O_5,M_r=340.33,单斜晶系,空间群P2(1)/c,a=0.86071(17)nm,b=1.1167(2)nm,c=0.93826(2)nm,β=115.10(3)°,V=0.8166(3)nm~3,D_c=1.384 g/cm~3,Z=2,F(000)=356,μ(Mo Kα)=0.103 mm~(-1),final R=0.0359,wR=0.0998.初步生物活性实验结果表明,在200μg/mL浓度下,部分化合物对小麦和拟南芥的生长有一定的抑制作用,而部分化合物对玉米的生长有促进作用.
In order to find an efficient, low toxicity and low residual pesticide lead compounds, mimicking the active structure of natural inhibitor of AdSS enzyme, L-tyrosine was used as starting material to synthesize 24 new 5 - (4-hydroxybenzyl) -2,4-imidazolidinedione ester compounds 6a ~ 6x, their structures were confirmed by IR, ~ 1HNMR and elemental analysis.Compound 6m was determined by X-ray diffraction: C 18 (16) N_2O_5, M_r = 340.33, monoclinic space group P2 (1) /c,a=0.86071 (17) nm, b = 1.1167 (2) nm and c = 0.93826 = 115.10 (3) °, V = 0.8166 (3) nm ~ 3, D_c = 1.384 g / cm ~ 3, Z = , final R = 0.0359, wR = 0.0998. The preliminary bioassay results showed that some compounds inhibited the growth of wheat and Arabidopsis at a concentration of 200μg / mL, while some of the compounds had a promoting effect on the growth of maize .