THE ANALYTICAL CHEMISTRY OF ANTI-AIDS AGENTS

本项目的目标是研究和开发适用于 生物分析方法：(1)建立结构和纯度 潜在的抗艾滋病药物和新型抗病毒药物，(2)确定 物理、化学和生化性质，包括辛醇-水 这些化合物及其代谢物的分配系数，以及(3) 在生物样本中测量这些药物及其代谢物以 阐明药理并测定药代动力学。高- 重点介绍了高效液相色谱和质谱学。 技巧。含糖双脱氧核苷，包括2‘-F-Dda和 2‘-F-DDI和修饰的环糊精硫酸酯m-CDS71的前药 目前主要感兴趣的化合物。一种高灵敏度的高效液相色谱 生物样品的直接荧光衍生化分析 已被开发用于F-Dda的分析。腺苷的作用 前药激活中的脱氨酶也在调查中。

The objective of this project is the research and development of suitable bioanalytical methods to: (1) establish the structure and purity of potential anti-AIDS agents and new antiviral drugs, (2) determine physical, chemical and biochemical properties, including octanol-water partition coefficients, of these compounds and their metabolites, and (3) measure these drugs and their metabolites in biological samples to elucidate pharmacology and to determine pharmacokinetics. High- performance liquid chromatography and mass spectrometry are emphasized techniques. Sugar-fluorinated dideoxynucleosides, including 2'-F-ddA and prodrugs of 2'-F-ddI and the modified cyclodextran sulfate m-CDS71 are currently the compounds of primary interest. A high sensitivity HPLC assay involving direct fluorogenic derivatization of biological samples has been developed for the analysis of F-ddA. The role of adenosine deaminase in prodrug activation is also under investigation.