氟喹诺酮类药物与蛋白质相互作用的研究

运用荧光淬灭机理研究了氟喹诺酮类药物洛美沙星，氧氟沙星，衣诺沙星与3种蛋白质(牛血清蛋白，免疫球蛋白，胰蛋白酶)之间的相互作用，计算了两者之间的结合常数和结合位点数，根据实验当中所得的热力学参数确定了它们之间的作用类型，氟喹诺酮类药物的含量与其荧光强度呈现良好的线性关系，在此实验条件下测定了胶囊及人工合成样中洛美沙星和衣诺沙星的含量，其浓度范围分别为0．018～0．878和0．030～3．171μg／mL。     

Synthesis of 2,4-dibromo-5-fluorobenzonitrile

2,4-Dibromo-5-fluorobenzonitrile has been synthesized for the first time (81.5% yield). It may be used in synthesizing 2,4-dibromo-5-fluorobenzoic acid, the intermediates of fluoroquinolones. The ammoxidation procedure for preparation of the nitrile has been described in detail. Zheng Qiong: born in 1945, Associate professor     

LC-MS-MS测定河口及近岸海水中的氟喹诺酮类药物

建立了河口及近岸海水中氟喹诺酮类药物残留的固相萃取富集-高效液相色谱-串级质谱测定方法.以Waters HLB固相萃取（SPE）小柱富集水样中的氟喹诺酮类药物,用XDB-C18柱、乙腈、甲酸（体积分数为0.2%）水流动相进行分离,ESI正离子源、三重串级质谱及多反应监测模式（MRM）进行目标物的定性、定量测定.优化实验...     

两种氟喹诺酮类抗生素在酸碱中的光谱特性

氟喹诺酮类药物的结构形态光谱性质受酸碱度的影响非常显著,在强酸介质(pH＜3)中,氟喹诺酮为强阳离子,荧光和紫外强度较弱;当pH为3～4时,氟喹诺酮为两性离子形式,荧光强度和紫外强度最大,环丙沙星(CIP)的最大激发波长和最大发射波长分别为280和459 mm,诺氟沙星(NOR)为281和450 mm;当pH为中性时,氟喹诺酮为弱阴离子,光谱蓝移,同时强度降低;在碱性条件下,氟喹诺酮为阴离子,荧光和紫外强度随着pH的升高而降低,但光谱形状基本不变.     

Study on the fluorescence properties of some fluoroquinolones in various media

The fluorescence emission from fluoroquinolones is shown to be associated with the substituted quinoline portion of the molecule. Neutral, anionic, zwitterionic and cationic forms of the fluorophore are proposed to account for the fluorescent behavior in aqueous and organic media of different acidities. In aqueous solution a ground-state pKa was observed for NFX and CPFX from a study of the pH vs. fluorescence profile with excitation at 331 nm, the ground-state microscopic dissociation constents for NFX or CPFX were determined. The causes of fluorescence changing were explained. The optimum condition for the fluorimetric determination of NFX, CPFX is an acidic medium (pH=2.0∼4.0) with λ_ex=280 nm or 331 nm and λ_em=445 nm. Supported by the National Natural Science Foundation of China Huang Zuyun: born in Aug. 1963. Ph. D graduate student     

盐酸替马沙星的新法合成

以２,４－二氯－５－氯苯甲酰乙酸乙酯为原料,经缩合、胺化,环合、螯合,取代,水解及成盐反应合成盐酸替马沙星。经元素分析,红外光谱,质谱和核磁共振谱确证结构,总收率４５％。该工艺路线副反应少,产品纯度高。