THE ANALYTICAL CHEMISTRY OF ANTI-AIDS AGENTS

该项目的目标是研究和开发 合适的分析方法：（1）确定结构和纯度 潜在的抗艾滋病药物和新的抗病毒药物，（2）确定 物理、化学和生物化学性质，包括辛醇-水 这些化合物及其代谢物的分配系数，以及 (3)测量生物样品中的这些药物及其代谢物， 阐明药理学并确定药代动力学。 高- 重点介绍了高效液相色谱和质谱 技术. 目前感兴趣的化合物是双脱氧核苷 包括6-卤代-dd-嘌呤，2-NH 2 -6-卤代-dd-嘌呤，2 ′-F-dd-ara-A， 2 ′-F-dd-ara-I、2 ′-F-dd-ara-G、2 ′-F-dd-C、2 ′-F2-dd-ara-C和 6-取代-2 '-F-dd-嘌呤。 腺苷脱氨酶的作用 前药活化正在研究中。

The objective of this project is the research and development of suitable analytical 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. Compounds of current interest are dideoxynucleosides including 6-halo-dd-Purines, 2-NH2-6-halo-dd-Purines, 2'-F-dd-ara-A, 2'-F-dd-ara-I, 2'-F-dd-ara-G, 2'-F-dd-C, 2'-F2-dd-ara-C and 6-substituted-2'-F-dd-Purines. The role of adenosine deaminase in prodrug activation is under investigation.