CAJ | 학술논문

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,~1H NMR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 Ka)=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.
위료발현고효、저독、저잔류적농약선도화합물,모의AdSS매천연억제제적활성결구,이L-락안산위기시원료,경과관배화지화등반응합성료24개신적5-(4-간기변기)-2,4-미서람이동지계렬화합물6a～6x,타문적결구통과IR,~1H NMR화원소분석진행료학증.화합물6m경X사선연사측정:C_(18)H_(16)N_2O_5,M_r=340.33,단사정계,공간군P2(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 Ka)=0.103 mm~(-1),final R=0.0359,wR=0.0998.초보생물활성실험결과표명,재200μg/mL농도하,부분화합물대소맥화의남개적생장유일정적억제작용,이부분화합물대옥미적생장유촉진작용.
To develop novel pesticide lcad compounds with high activity,low toxicity and low residue,24 novel 5-(4-hydroxybenzyl)-2,4-imidazolidinedione(hydantoin)esters were synthesized with cyclization and esterification using L-tyrosine as raw material by simulating the structure of natural inhibitor against AdSS synthetase,and structurally confirmed by m.P.,IR,~1H NMR and elemental analysis.X-ray diffraction analysis of 6m was studied as C_(18)H_(16)N_2O_5,M_r=340.33,monoclinic,space group 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 Ka)=0.103 mm~(-1),final R=0.0359,wR=0.0998.The preliminary bioassay results indicated that some of these compounds had certain inhibition activities against Triticum aestivum and Arabidopsis thaliana,while some of them could promote the growth of Zea mays at the concentration of 200μg/mL.