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通过取代苯氧异丁酸与12-(羟基亚氨基)十五内酯的反应,合成了取代苯氧异丁酰氧亚氨基十五内酯,并测定了其对苋菜的除草活性。所有化合物均经过1H NMR、13C NMR和元素分析确证。初步的生物活性测定结果表明,目标化合物 Ⅲa~Ⅲd 的EC50值分别为34.570、46.492、55.385、50.114 mg/L,其活性比对照药剂2,4-D(117.325 mg/L)高,而比苯磺隆(22.381 mg/L)低。 相似文献
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以莰烯醛肟与卤代物为原料经亲核取代反应合成了9个未见报道的莰烯醛O-取代肟类化合物,分别为2-(3,3-二甲基双环[2.2.1]庚-2-亚基)乙醛O-苄基肟(2a)、2-(3,3-二甲基双环[2.2.1]庚-2-亚基)乙醛O-丁基肟(2b)、2-(3,3-二甲基双环[2.2.1]庚-2-亚基)乙醛O-(4-氯丁基)肟(2c)、2-(3,3-二甲基双环[2.2.1]庚-2-亚基)乙醛O-(3-溴苄基)肟(2d)、2-(3,3-二甲基双环[2.2.1]庚-2-亚基)乙醛O-(4-叔丁基苄基)肟(2e)、2-(3,3-二甲基双环[2.2.1]庚-2-亚基)乙醛O-(4-氯苄基)肟(2f)、2-(3,3-二甲基双环[2.2.1]庚-2-亚基)乙醛O-(4-氰基苄基)肟(2g)、2-(3,3-二甲基双环[2.2.1]庚-2-亚基)乙醛O-(2,6-二氯苄基)肟(2h)、2-(3,3-二甲基双环[2.2.1]庚-2-亚基)乙醛O-(邻氟苄基)肟(2i)。利用FT-IR、GC-MS、1H NMR以及13C NMR对产物结构进行了表征。以化合物2a为例,探索了不同工艺条件对产物得率的影响,在甲苯为溶剂,n(莰烯醛肟)∶n(氯化苄)∶n(四丁基溴化铵)为1.0∶1.8∶0.08,反应温度为60℃,反应时间为20 h的最佳工艺条件下,产物的得率为84.1%。通过体外抗肿瘤活性测试,探讨了化合物2a^2i对肝癌细胞HepG2和人乳腺癌细胞MCF7的抑制作用,结果表明:化合物2b对HepG2细胞的抑制作用较好,其半数抑制浓度(IC 50)值为36.3μmol/L;化合物2d、2h、2i对MCF7有一定的抑制作用,其中化合物2h对MCF7的抑制作用较好,其IC50值为19.2μmol/L。 相似文献
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[目的] 研究结石通片对小鼠的急性毒性作用,对健康大鼠的利尿作用,以及对乙二酰胺致大鼠肾结石的调节作用。[方法] 取ICR小鼠40只,雌、雄各半,随机分为对照组与给药组,每组20只,观察结石通片给药前后小鼠的体重变化和死亡情况;另取SD大鼠36只,雌、雄各半,分为对照组、低剂量组(给予5%结石通片溶液)和高剂量组(给予10%结石通片溶液),统计各组大鼠24 h排尿量;并采用42只雄性SD大鼠,考查结石通片对给予乙二酰胺(2%掺喂)后大鼠体重、肾重和肾重比的影响。[结果] 给予结石通片溶液后,连续观察7 d,小鼠的各项生理活动未见明显异常,给药组与对照组相比体重差异不显著(P>0.05);与对照组比较,给予结石通片溶液后大鼠24 h内排尿量明显增加(P<0.01);与对照组比较,给药组随着给药剂量的增加,结晶和结石的数量极显著(P<0.01或P<0.001)减少,形成结石的动物数量极显著(P<0.01或P<0.001)减少。[结论] 结石通片对小鼠无明显急性毒性作用,对大鼠利尿作用明显,并对乙二酰胺致大鼠肾结石具有明显抑制作用。 相似文献
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Holm BR 《Veterinary dermatology》2003,14(4):189-195
Ninety-nine dogs diagnosed with generalized demodicosis were treated with milbemycin oxime. Cases diagnosed before two years of age were classified as juvenile-onset (53%) and those diagnosed after two years of age as adult-onset (47%). Dogs were considered cleared of mites when none could be demonstrated in scrapings and cured if no relapse was seen for 12 months. Eighty-five per cent (84/99) were cured with milbemycin oxime used for 1-6 months (mean 2.3 months) at a dosage of 0.5-1.6 mg kg-1 body weight (mean 0.75 mg kg-1). No significant difference in dosage or treatment time was seen between juvenile and adult cases. Chance of cure was significantly better in young animals (cured cases mean age 2.97 years) than in older animals (not cured cases mean age 8.02 years). Start of treatment early in the course of disease gave a significantly better chance of cure. Cases with severe pododemodicosis had less chance of a cure (9/11 not cured). 相似文献
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Claudia Böhm Manuela Schnyder Stig Milan Thamsborg Caryn M. Thompson Candace Trout Sonja Wolken Beate Schnitzler 《Veterinary parasitology》2014,199(3-4):272-277
Angiostrongylus vasorum is an increasingly reported parasite in Europe that develops in dogs after ingestion of infective third stage larvae (L3) that reside in gastropod molluscs which are needed to complete the parasite's life-cycle. Infection can produce a diversity of clinical signs, determined by involvement of the respiratory, neurological, and/or coagulation system, with a likely fatal outcome in the absence of treatment. Few drugs have been shown to reliably prevent infection, and data on treatment of infections is limited. A controlled, randomized, partially blinded laboratory study was therefore executed to evaluate the efficacy and safety of a combination tablet of spinosad/milbemycin oxime in dogs inoculated with approximately 250 A. vasorum L3. Sixteen healthy nematode free adult dogs were randomly allocated to two study groups of 8 dogs each. Thirty days post inoculation (dpi) all dogs in the fed state were treated: dogs in group B were treated with spinosad and milbemycin oxime at the dose rates of 45–60 mg/kg and 0.75–1.0 mg/kg bodyweight, respectively, approximately the lower half portion of the expected full unit dose range; dogs in group A were treated with placebo tablets. All dogs were euthanized and necropsied 56–58 dpi. The heart and lungs were examined to determine the presence of A. vasorum. All placebo group dogs were infected at necropsy with counts ranging from 22 to 98 adult worms and a geometric mean worm count of 55.2. In contrast, the geometric mean worm count in the spinosad/milbemycin oxime group was 0.7 with worm numbers ranging from 0 to 8. The results of this study demonstrate that a single treatment with the tablet combination of spinosad and milbemycin oxime administered 30 dpi provided 98.8% preventive efficacy against development of adult A. vasorum infections. Monthly treatments with spinosad and milbemycin oxime have the potential to prevent the establishment of infections with A. vasorum in dogs. 相似文献
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对紫外-可见分光光度法测定阿苯达唑片含量的不确定度进行评定以及测量过程中各种不确定度来源进行分析与评估,含量测定结果可表示为(95.7±2.0)%(k=2)。结果表明,仪器的吸光度、重量差异、称样量和移液管的体积引入的不确定度为测量结果不确定度的主要影响因素。 相似文献
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为完善银翘片质量标准,采用高效液相色谱法对银翘片中牛蒡苷的含量测定进行了研究。色谱柱为C18(4.6mm×250mm,5μm),流动相为乙腈-0.1%冰乙酸溶液(25:75),检测波长为280nm,流速1mL/min,柱温25℃,进样量10μL。牛蒡苷进样浓度在0.1~2mg/mL范围内与峰面积呈良好的线性关系(r=0.9999);样品平均回收率为96.5%(n=6),RSD为1.3%。本方法简便、准确度高、重复性好,为进一步控制银翘片的质量提供了依据。 相似文献