THE ANALYTICAL CHEMISTRY OF ANTI-AIDS AGENTS

抗艾滋病药物的分析化学

• 批准号: 3853162
• 负责人: J A KELLEY
• 金额: --
• 依托单位: DIVISION OF CANCER TREATMENT
• 依托单位国家: 美国
• 资助国家: 美国
• 起止时间: 至
• 项目状态: 未结题
• 来源: https://reporter.nih.gov/project-details/3853162
• 关键词: 2'3' dideoxynucleoside; AIDS; AIDS therapy; adenosine deaminase; analytical chemistry; antiAIDS agent; antiviral agents; chemical structure function; drug design /synthesis /production; drug metabolism; gas chromatography; high performance liquid chromatography; mass spectrometry; nucleoside analog; pharmacokinetics; purine analog

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.

该项目的目的是研究和发展 合适的分析方法：（1）建立结构和纯度 潜在的抗AIDS剂和新的抗病毒药，（2）确定 物理，化学和生化特性，包括辛醇水 这些化合物及其代谢物的分区系数，以及 （3）在生物样品中测量这些药物及其代谢物 阐明药理学并确定药代动力学。 高的- 强调性能液相色谱和质谱法 技术。 当前感兴趣的化合物是二乙氧基核苷 包括6-halo-dd-purines，2-NH2-6-HALO-DD-PURINE，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-purines。 腺苷脱氨酶在 前药激活正在研究中。