芳氨基脲类化合物单侧脱氢制取新型偶氮化合物

在丙酮溶剂中 ,利用氧化剂CAN将 8种芳氨基脲类化合物高产率地氧化为新型偶氮化合物 ,反应条件温和 ,现象明显 ,产物容易分解 .     

Microwave-assisted synthesis, anticonvulsant activity and quantum mechanical modelling of N-（4-bromo-3-methylphenyl） semicarbazones

Objective： To study the effect of halo substitution on disubstituted aryl semicarbazones on the anticonvulsant potential and model the activity based on quantum mechanics. Methods： A series of twenty-six compounds of N^4-（4-bromo-3-methylphenyl） semicarbazones were synthesized and evaluated for the anticonvulsant activity in the maximal electroshock seizure （MES） and subcutaneous pentylenetetrazole （scPTZ） seizure threshold tests. Some potential compounds were also tested in the subcutaneous strychnine （scSTY） and subcutaneous picrotoxin （scPIC） seizure threshold tests. The synthesized compounds were tested for behavioral impairment and CNS （central nervous system） depression in mice. Quantum mechanical modelling was carried out on these compounds to gain understanding on the structural features essential for activity. Results： Some compounds possessed broad spectrum anticonvulsant activity as indicated by their effect in pentylenetetrazole, strychnine, picrotoxin and maximal electroshock seizures models in resemblance to other aryl semicarbazone derivatives reported earlier. The higher the difference in HOMO （highest occupied molecular orbital） and LUMO （lowest unoccupied molecular orbital） energy levels was, the greater was the activity profile. Conclusion： The pharmacophoric requirements for compounds to exhibit anticonvulsant activity that includes one aryl unit in proximity to a hydrogen donor-acceptor domain and an electron donor have been justified with the molecular orbital surface analysis of the synthesized compounds.     

含开链冠醚基二芳醛缩氨基(硫)脲的合成研究〔Ⅱ〕

合成了六个含开链冠醚基的缩氨基(硫)脲类化合物,并用IR、HWMR、MS等谱确证了其结构。     

含硫脲基schiff碱型配体的合成研究──含开链醚基二芳醛缩4—烯丙基—3—硫代氨基脲的合成

由含开链冠醚基的二芳醛与４—烯丙基—３—硫代氨基脲缩合，合成三种含硫ｓｃｈｉｆｆ碱基开链冠醚类配体，并初步研究了其与一些盆属离子的配位性能。     

1-苯基-3-甲基-4-苯甲酰基吡唑啉酮-5双缩对称二氨基硫脲的合成

合成了新的含硫希夫碱配体 1-苯基 - 3-甲基吡啉酮 - 5双缩对称二氨基硫脲 ,通过元素分析、红外光谱对其配体进行了表征     

Synthesis and evaluation of 4-substituted semicarbazones of levulinic acid for anticonvulsant activity

Objective: A series of 4-aryl substituted semicarbazones of levulinic acid (4-oxo pentanoic acid) was designed and synthesized to meet the structural requirements essential for anticonvulsant activity. Methods: All the compounds were evaluated for anticonvulsant activity. Anticonvulsant activity was determined after intraperitoneal (i.p.) administration to mice by maximal electroshock (MES) and subcutaneous metrazol (ScMet) induced seizure methods and minimal motor impairment was determined by rotorod test. Results: A majority of the compounds exhibited significant anticonvulsant activity after intraperitoneal administration. In the present study 4-(4'-fluoro phenyl) levulinic acid semicarbazone emerged as the most active molecule, showing broad spectrum of activity with low neurotoxicity. Unsubstituted levulinic acid semicarbazone was found to be inactive in all the screens. Conclusion: The results obtained validate the hypothesis that presence of an aryl group near the semicarbazone moiety is essential for anticonvulsant activity. The results also indicate that the hydrophilic-hydrophobic site can accommodate hydrophilic groups.     

含开链冠醚基二芳醛缩4-烯丙基-3-硫代氨基脲的合成

由含开链冠醚基的二芳醛与4-烯丙基-3-硫代氨基脲缩合,合成三种含硫schiff碱型开链冠醚类配体,并初步研究了其与一些金属离子的配位性能。     

聚丙烯—二苯氨基脲树脂分离富集碘—四氯化碳萃取光度法测定矿石中的金

研究了聚丙烯-二苯氨基脲树脂萃取柱富集金,洗脱后采用I2一CCl4萃取光度法测定矿石中的痕量金.通过方法的回收率试验测定金的回收率为93%-107%.与其他测定方法进行比较,此测定方法效果较好.     

脑内GABA能神经元对红藻氨酸中枢性心血管效应的影响

采用侧脑室微量注射方法证明,谷氨酸(G1u)受体亚型激动剂红藻氨酸(KA)可剂量依赖性地增加大鼠血压和心率。预先给予GABA合成抑制剂氨基脲(SCZ)140mg/kg ip或GABA拮抗剂印防已毒(PIC)1mg/kg iv均可明显增强KA的作用;而GABA转氨酶抑制剂氨氧乙酸(AOAA)25μg/rat icv明显减弱KA的作用。结果表明,脑内GABA能神经元功能影响KA的中枢性心血管效应。从而推测:脑内GABA能神经元与Glu能神经元之间相互作用,共同参与心血管活动的中枢调节。