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1.
为了合成两种具有抑菌活性的1,4-二氧喹醛酸酯,即1,4-二氧喹喔啉-3-甲基-2-甲酸苯酯和1,4-二氧喹喔啉-3-甲基-2-甲酸肉桂酯,以苯并呋咱为原料,经Beirut反应、酯交换反应,合成了两种喹醛酸酯;1,4-二氧喹喔啉-3-甲基-2-甲酸苯酯合成产率为29.3%,1,4-二氧喹喔啉-3-甲基-2-甲酸肉桂酯合成产率为18.3%。两种1,4-二氧喹醛酸酯对大肠杆菌、金葡萄球菌、青霉菌和枯草杆菌均有明显的抑菌活性。通过测定产物的熔点和光谱分析证明系为所合成的目标产物。  相似文献   

2.
用水杨醛、1,4—二氧喹喔啉—2—甲醛与邻苯二胺反应制备了二种单席夫碱中间体,用2种中间体、8种取代芳香胺与1,4—二氧喹喔啉—2—甲醛反应合成了10种新席夫碱。用元素分析法、MS法(质谱法)、IR法(红外吸收光谱分析法)和1HNMR法(核磁共振氢谱法)对这些新席夫碱的结构进行了表征。用这些新席夫碱对鸡进行了促生长活性实验,实验结果显示了苯胺、对—氯苯胺和对—乙酰胺基苯胺的席夫碱有明显促进鸡生长的作用,相对增重率在30%以上。  相似文献   

3.
喹胺醇(Kuianchun)是一种新型药物饲料添加剂,其母体结构为喹噁啉-1,4-二氧化物,和喹烯酮、喹赛多等一样均属结构创新类药物,由中国农业科学院兰州畜牧与兽医研究所研制而成.  相似文献   

4.
2-乙酰基-3-甲基喹噁啉-1,4-二氧化物的合成工艺研究   总被引:1,自引:0,他引:1  
研究了2-乙酰基-3-甲基喹噁啉-1,4-二氧化物的合成工艺.以邻硝基苯胺为起始原料,经过氧化反应和Beirut反应,以86%的总收率制得产物2-乙酰基-3-甲基喹噁啉-1,4-二氧化物.反应条件温和,操作简单,收率高,具有工业应用价值.  相似文献   

5.
<正>喹噁啉衍生物(quinoxalines)是一类重要的苯并吡嗪类杂环化合物,喹噁啉环上的2个N原子氧化形成的喹噁啉-1,4-二-N-氧化物(quinoxaline 1,4-di-N-oxides,qdNOs)具有多种生物学活性,包括抗细菌和抗念珠菌活性、促生长活性、抗虫活性和抗肿瘤活性等[1],在医药和农业中有着重要的应用价值和前景。含QdNO结构的动物用喹噁啉类兽药  相似文献   

6.
为了合成一种有抑菌活性的新喹喔啉衍生物,即3-甲基-2-乙酰苯腙喹喔啉1,4-二氧物,以邻硝基苯胺为基本原料,经氧化反应,Beirut反应和加成缩合反应,制得目标产物,产率73.5%。用红外光谱法(IR)、质谱法(MS)和核磁共振谱法(NMR)对产物结构进行表征,证明合成产物为目标产物。并通过抑菌测试发现,新化合物对大肠杆菌、枯草杆菌、金葡萄球菌和青霉菌均有明显的抑菌活性,为今后开展喹喔啉及其衍生物的抗菌药用研究奠定基础。  相似文献   

7.
正1喹乙醇是什么?喹乙醇又名喹酰胺醇,属于喹噁啉类。于1965年由德国拜耳公司(Bayer)以邻硝基苯胺为原料合成的一种饲料添加剂,当时因其性能稳定、效果显著、用量少、被当做人工合成的喹噁啉化合物中一种理想的畜禽抗菌促生长剂。喹乙醇的化学名称为2-[N-(2-羟基-乙基)-氨基甲酰]-3-甲基-喹噁啉-1,4-二氧化物。本品为浅黄色结晶性粉末,无臭,  相似文献   

8.
对磺胺喹噁啉钠采用硅胶GF254板为固定相,以正丁醇-浓氨水(15∶3)为展开剂,用薄层色谱鉴别中兽药散剂中磺胺喹噁啉钠分离较好,斑点显色清晰且无干扰,可用于中药散剂中非法添加物磺胺喹噁啉钠的快速筛选。采用C18柱为固定相,以甲醇-乙腈-水-冰乙酸(2∶2∶9∶0.2)为流动相,紫外检测波长为270 nm。液相色谱鉴别中药散剂中非法添加磺胺喹噁啉钠分离良好,无干扰峰,可用于中兽药散剂中非法添加物磺胺喹噁啉钠的鉴别。  相似文献   

9.
痢菌净又名乙酰甲喹,化学名为3-甲基-2-乙酰基喹噁啉-N-1,4-二氧化物,是我国研制的具有自主知识产权的兽用卡巴氧类抗菌药品。为鲜黄色结晶或黄色粉末。无臭,味微苦。在水、甲醇中微溶。本品因抗菌谱广,价格低廉且不易产生耐药性,故在畜牧养殖业上应用广泛。但在使用过程中常因超剂量应用或过量误服而导致中毒现象发生,造成严重的损失。  相似文献   

10.
正喹乙醇(Olaquindox)属于喹噁啉类药物,又被称为喹酰胺醇、倍育诺,商品名有灭霍灵、灭败灵、快育灵等,是1965年德国拜耳公司以邻硝基苯胺为原料合成的饲料药物添加剂,在国内北京营养源研究所1981年首次研制成功。喹乙醇的化学名称为:2-[N一(2-羟基一乙基)-氨基甲酰]-3-甲基一喹噁啉-1,4一二氧化物,分子式C12H13N3O4,为浅黄色结晶性粉末,无臭,味苦,溶于热水,微溶于  相似文献   

11.
This study aimed to establish a standard dose and sample collection time for 13C phenylalanine and 13C-Dipeptide breath test in horses. To evaluate dose-dependent effects, healthy horses received 2.5 mg/kg, 5 mg/kg, and 10 mg/kg 13C phenylalanine dissolved in 1 ml/kg distilled water and 1.25 mg/kg, 2.5 mg/kg, and 5 mg/kg 13C dipeptide dissolved in 2 ml/ kg distilled water. Tmax was observed during the sample collection time. For 13C phenylalanine, the standard deviation of Cmax at 5 mg/kg was lower than that of 10 mg/kg. For 13C dipeptide, the standard deviation of Tmax was the lowest at 5 mg/kg. This study revealed that an optimal dose for breath tests with 13C phenylalanine and 13C dipeptide may be 5 mg/kg in horses.  相似文献   

12.
ABSTRACT

1. The aim was to evaluate the acaricidal effects of pure active components of essential oils against poultry red mite (Dermanyssus gallinae) as an alternative to chemical acaricides (organophosphates and pyrethroids).

2. The toxicities of five pure active components of essential oils (eugenol from clove bud, eucalyptol from rosemary, limonene from citrus fruits, linalool from lavender and cinnamaldehyde from cinnamon) were tested on D. gallinae females in an impregnated paper assay.

3. The active substances were dissolved in water and Tween 20 and applied at concentrations ranging from 0.002 to 0.06 µl/cm2. Toxicity was expressed as a lethal dose (LD50 or LD90).

4. The highest mortality was observed with eugenol. The LD90 was estimated to be 5.1 µg/cm2 for this substance, followed by cinnamaldehyde, the LD90 of which was estimated to be 11.0 µg/cm2. Limonene and eucalyptol were generally less effective in controlling D. gallinae.  相似文献   

13.
Bovine immunodeficiency-like virus (BIV) was passagedin vivo by intraperitoneal transfusion of ovine whole blood. Prior to transfusion, the recipient sheep were given sodium thioglycolate intraperitoneally to induce mild non-suppurative inflammation. The anti-BIV antibody response, haematology, and peripheral blood lymphocyte subsets (B, , CD2+, CD4+ and CD8+) of recipient sheep were assessed for one year following transfusion. Passaging was successful since serum anti-BIV antibody responses were detected in 5 of the 6 recipient sheep; 1 of the 5 remained seropositive throughout the study. Lentivirus was not isolated from the recipient sheep, but provirus was detected by the polymerase chain reaction in DNA from peripheral blood leukocytes in 3 of the 5 sheep that seroconverted. In the BIV-inoculated sheep, neutrophils and eosinophils were significantly increased (p0.05) at 3 months and between 6 and 8 months postinoculation, respectively. B, CD2+ and CD4+ cells and the CD4+/CD8+ ratios were significantly increased (p0.05) 2 months postinoculation. Mild, transient haematological changes occurred in BIV-exposed sheep, but illness was not detected in the year.  相似文献   

14.
高寒灌丛土壤温室气体释放对添加不同形态氮素的响应   总被引:4,自引:0,他引:4  
为探索不同形态氮素输入对青藏高原高寒灌丛土壤CO2、N2O和CH4排放的影响,采集青藏高原东部金露梅高寒灌丛土壤,设置1个对照(CK)和3个添加不同形态氮素的处理(NH4Cl,NH4NO3,KNO3),在实验室恒温15℃下进行培养,分析了土壤CO2、N2O和CH4的释放量以及土壤NH4+,NO3-和可溶性有机碳(DOC)含量。结果表明:1)所有氮素处理抑制了高寒灌丛土壤CO2的排放,土壤CO2排放量与DOC浓度呈显著正相关关系;2)所有氮素处理显著增加了土壤N2O的排放,而且以添加NO3--N增加的N2O最为显著;3)高寒灌丛土壤N2O的产生过程以反硝化作用为主;4)添加不同形态氮素对高寒灌丛土壤CH4吸收没有显著影响。5)不同形态氮素施入后,高寒灌丛土壤温室气体全球增温潜能(GWP)顺序:KNO3>NH4NO3>NH4Cl>CK。  相似文献   

15.
The purpose of this study was to determine the plasma pharmacokinetics (PK) and toxicity of zebularine, an oral cytidine analog with demethylating activity, in dogs. Plasma zebularine concentrations were determined by HPLC‐MS/MS following an oral zebularine dose of 8 or 4 mg kg?1. Plasma zebularine clearance was constant. Mean maximum concentration (Cmax) was 23 ± 4.8 and 8.6 ± 1.4 µM following 8 and 4 mg kg?1, respectively. Mean half‐life was 5.7 ± 0.84 and 7.1 ± 2.1 following 8 and 4 mg kg?1, respectively. A single 8 mg kg?1 dose was well tolerated. Daily 4 mg kg?1 treatment in three laboratory dogs resulted in grade 4 neutropenia (n = 3), grade 1 anorexia (n = 2) and grade 1 or 2 dermatologic changes (n = 2). All adverse events resolved with supportive care. A 4 mg kg?1 dose every 21 days was well tolerated. A follow‐up dose escalation study is in progress with a lower starting dose.  相似文献   

16.
The incidence and location of CD2+, CD4+, CD8+ and γ/δ T lymphocytes and IgM+ B lymphocytes were studied in the intestinal lymph nodes in 1-week, 1-month, 3-month and 7-month-old goats, using monoclonal antibodies and immuno-histochemical methods. The cortical area of the intestinal lymph nodes in 1-week-old animals contains only primary follicles occupied by IgM+ B lymphocytes and some CD2+CD4+ T lymphocytes. In goats older than 1 month, secondary follicles, that increased in number and size with age, were observed; the light zone of the germinal centre was occupied by IgM+ lymphocytes and some CD2+ and CD4+ T lymphocytes. In the other compartments of the lymph nodes, B lymphocytes were scarce, their number increasing with age in the medulla and diminishing in the paracortex. The numerous CD2+ T lymphocytes in the interfollicular area increased in number in the paracortical area of the 7-month-old goats, simultaneously with an increase in the MHC II+ dendritic cells and the CD4/CD8 ratio, which was greater than 1. The γ/δ T lymphocytes represented a minor subpopulation scattered through the lymph nodes.  相似文献   

17.
Differentially extended specific protection by two commercial vaccines against Yersinia ruckeri serotype O1 biotype 2 was studied following 30 s immersion exposure. Rainbow trout were challenged intra-peritoneally (i.p.) with Y. ruckeri serotype O1, biotype 2 (≈106 to 107 CFU/fish) at 4, 6 and 8 months after vaccination with vaccines containing either biotype 1 (AquaVac® ERM) or both biotypes 1 and 2 (AquaVac® RELERA?). The specific pattern of vaccine-mediated protection was evaluated by relative percentage survival (RPS) analysis at 4 and 6 months post-vaccination and by obtaining gross pathological observations at 4 and 8 months respectively. We determined specific significant and superior protection in terms of increased survivability in AquaVac® RELERA? vaccinated fish and observed correspondingly fewer pathological changes. The challenge trials indicated a longer protection for at least 6 months without any booster vaccination. A specific and adaptive response induced by AquaVac® RELERA? vaccine against Y. ruckeri biotype 2 was clearly indicated. In addition, some degree of cross protection rendered by AquaVac® ERM containing biotype 1 during infection with Y. ruckeri biotype 2 was also noted.  相似文献   

18.
ObjectiveTo establish the correlation between the bispectral index (BIS) and different rates of infusion of propofol in dogs.Study designProspective experimental trial.AnimalsEight adult dogs weighing 6–20 kg.MethodsEight animals underwent three treatments at intervals of 20 days. Propofol was used for induction of anesthesia (10 mg kg−1 IV), followed by a continuous rate infusion (CRI) at 0.2 mg kg−1 minute−1 (P2), 0.4 mg kg−1 minute−1 (P4) or 0.8 mg kg−1 minute−1 (P8) for 55 minutes. The BIS values were measured at 10, 20, 30, 40, and 50 minutes (T10, T20, T30, T40, and T50, respectively) after the CRI of propofol was started. Numeric data were submitted to analysis of variance followed by Tukey test (p < 0.05).ResultsThe BIS differed significantly among groups at T40, when P8 was lower than P2 and P4. At T50, P8 was lower than P2. The electromyographic activity (EMG) in P2 and P4 was higher than P8 at T40 and T50.ConclusionsAn increase in propofol infusion rates decreases the BIS values and EMG.  相似文献   

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