Access to 18F‐labelled isoxazoles by ruthenium‐promoted 1,3‐dipolar cycloaddition of 4‐[18F]fluoro‐N‐hydroxybenzimidoyl chloride with alkynes

4‐[¹⁸F]Fluoro‐N‐hydroxybenzimidoyl chloride (¹⁸FBIC), an ¹⁸F‐labelled aromatic nitrile oxide, was developed as building block for Ru‐promoted 1,3‐dipolar cycloaddition with alkynes. ¹⁸FBIC is obtained in a one‐pot synthesis in up to 84% radiochemical yield (RCY) starting from [¹⁸F]fluoride with 4‐[¹⁸F]fluorobenzaldehyde (¹⁸FBA) and 4‐[¹⁸F]fluorobenzaldehyde oxime (¹⁸FBAO) as intermediates, by reaction of ¹⁸FBAO with N‐chlorosuccinimide (NCS). ¹⁸FBIC was found to be a suitable and stable synthon to give access to ¹⁸F‐labelled 3,4‐diarylsubstituted isoxazoles by [Cp*RuCl(cod)]‐catalysed 1,3‐dipolar cycloaddition with various alkynes. So the radiosynthesis of a fluorine‐18–labelled COX‐2 inhibitor [¹⁸F] 1b , a close derivative of valdecoxib, was performed with ¹⁸FBIC and 1‐ethynyl‐4‐(methylsulfonyl)benzene, providing [¹⁸F] 1b in up to 40% RCY after purification in 85 minutes. The application of ¹⁸FBIC as a building block in the synthesis of ¹⁸F‐labelled heterocycles will generally extend the portfolio of available PET radiotracers.     

社区获得性肺炎患者联合监测肺炎支原体与肺炎衣原体的临床意义

目的 探讨联合监测肺炎支原体(Mp)和肺炎衣原体(Cp)对社区获得性肺炎(CAP)患者的临床意义.方法 选取2012年2月至2014年10月我院收治的CAP患者1 580例,监测患者咽拭子标本中Mp、Cp,培养并鉴定其主要病原菌,比较不同抗感染方案的疗效.结果 CAP病原体以Mp (30.0%)、肺炎链球菌(15.9%)、流感嗜血杆菌(12.9%)、Cp (10.1%)比例最高,且同时合并2种病原体感染者较为多见(10.1%);治疗中β-内酰胺类药物使用频率最高(76.71%);β-内酰胺类联合大环内酯类或联合氟喹诺酮类药物对CAP治愈率(66.72%)显著高于单独应用β-内酰胺类药物治疗(56.73%,P<0.01);单用β-内酰胺类药物治疗与应用β-内酰胺类联合氟喹诺酮类(65.4%)或大环内酯类药物(68.5%)对单纯Mp或Cp感染CAP治愈率比较差异均无统计学意义(P>0.05),而在细菌合并Mp或Cp感染时,联合用药治愈率(69.7%)明显高于单用β-内酰胺类药物(44.4%),差异有统计学意义(P<0.05).结论 CAP患者感染Mp与Cp较多见,β-内酰胺类药物是常用治疗药物,β-内酰胺类联合大环内酯类或氟喹诺酮类药物可提高患者治愈率,Mp与Cp联合检测对于敏感抗生素的选择及疗效的提高具有重要临床意义.     

脑性瘫痪患儿家庭生活质量研究

目的:脑性瘫痪(简称脑瘫)患儿的治疗、教育、智力开发及本身生活质量与其监护人的生活质量关系密切。调查脑瘫患儿家长的生活质量,以便实施正确引导,使之能配合脑瘫患儿的全面干预治疗。方法:用“医院焦虑抑郁量表”对50例脑瘫患儿监护人与50例急性病患儿监护人进行配对衡量对照,并就患儿现状、家庭情况、对孩子患病态度、患病对家庭生活影响以及由此带来的家长对治疗的态度等方面进行流行病学调查研究。结果:脑瘫患儿监护人焦虑抑郁量表总评分(AD):19.1±2.3,其中焦虑评分(A):10.1±2.2,抑郁评分(D):8.9±0.7。对照组监护人焦虑抑郁量表总评分(AD):5.7±1.4,焦虑评分(A):3.4±1.3,抑郁评分(D):2.4±1.0,两组间各项评分差异均有显著性意义(t=35.092,18.529,39.056,P均<0.001)。结论:脑瘫患儿家长普遍存在焦虑抑郁情绪、生活质量下降,应给与适当心理指导。     

Response variability of human brain tumors to AZQ in tissue culture

Summary In a series of 28 glioma-derived cell cultures and 6 non-gliomatous CNS tumors, AZQ has been found to have varying degrees of growth inhibiting or cytotoxic activity in nearly all lines tested at doses greater than 100 mcg/ml. At dose levels comparable to the clinically achieved levels (1 mcg/ml), AZQ was found to have a cytotoxic effect in 8 of 28 glioma-derived and 2 of 6 non-gliomatous cell lines tested. These findings suggest that AZQ has activity against certain glioma-derived cells in culture at a response ratio similar to that seen in vivo. There, appear to be significant differences in the degree of responsiveness in different patients' tumor cells which can be detected in vitro prior to clinical treatment.Address for offprints: National Institutes of Health, Surgical Neurology Branch, NINCDS, 9000 Rockville Pike, 10A-3E68, Bethesda, Maryland 20892, USA     

小儿肺炎肺炎支原体与衣原体感染状况分析

目的:对小儿肺炎肺炎支原体(Mp)、肺炎衣原体(Cp)感染状况调查,探讨其流行规律,制定可行的防治措施。方法:采用聚合酶链反应(PCR)技术检测742例肺炎患儿Mp、Cp的感染。结果:742例肺炎患儿Mp的阳性检出率随年龄的增长而增加,大年龄组明显高于小年龄组(P<0.01)。3个年龄组Cp及Mp+CP阳性检出率差异均无显著性(P>0.05)。Mp、Cp阳性率高峰分布在1、4季度,各季节感染率差异有显著性(P<0.05)。Mp+Cp混合感染各季节之间无明显差异(P>0.05)。结论:Mp感染随年龄的增长而增加,多见于大年龄组,Mp、Cp感染年龄有提前趋势,不同性别之间的感染率没有明显差异,感染季节以1、4季度多见。     

药物动力学模型的C_p选择法

目的:为药物动力学(PK)模型的选择提供一个新定量指标。方法:将多元回归分析中选择“最优”回归模型的统计量Cp的计算公式赋予新含义使之适用于PK房室模型选择。结果:经实例计算,与AIC准则判定的PK模型相同,但Cp选择法更为灵敏。     

吸光系数法测定二氯二茂钛原料药的含量

采用吸光系数法对二氯二茂钛原料药进行含量测定。３９１ｎｍ处测得Ｅ１％１ｃｍ＝９８．３２,平均回收率为９８．７７％～１０１．７４％。相对标准差ＲＳＤ＝０．１２％～０．６６％。测定不同温度,湿度下放置不同时间原料药的含量。与工作曲线法相比。两者之间无显著性差异。     

饰瓷对不同材料基底冠边缘适合性的影响

目的:比较金合金、纯钛、镍铬合金基底冠饰瓷前后的冠边缘适合性的变化以及临床意义。方法:在按统一标准机加工预备的树脂基牙模型上分别制作3组共24个全冠蜡形,严格按金合金、纯钛以及镍铬合金3种材料的要求分别进行铸造。对所得铸件在就位完全后,分别测量基底冠的颊侧、远中、腭侧以及近中边缘中点至基牙预备终止线的垂直距离,然后分别以相匹配的瓷粉饰瓷,再测量上述4点,得到饰瓷后的边缘间隙数据。以金合金组为对照组,纯钛组和镍铬合金组为实验组,用SAS统计软件对测量所得数据进行统计学分析。结果:金合金、纯钛以及镍铬合金各组饰瓷后4个点位的边缘间隙较饰瓷前均有明显的增大,各组差值有统计学差异,其中纯钛组4点间隙差值明显小于镍铬合金组和金合金组,而镍铬合金组与金合金组之间4点的间隙差值无明显差异。以上3组的饰瓷后的各点边缘间隙均小于120μm。结论:饰瓷对纯钛基底冠边缘适合性的影响最小。3组基底冠饰瓷后的冠边缘适合性均在临床可接受的范围内。