SYNTHESIS OF CONGENERS AND PRODRUGS--ANTI-AIDS

同系物及前药的合成--抗艾滋病

• 批准号: 3615900
• 负责人: MARK CUSHMAN
• 金额: $ 16.28万
• 依托单位: PURDUE UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 1988
• 资助国家: 美国
• 起止时间: 1988-06-30 至 1991-06-29
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3615900
• 关键词: antiAIDS agent; drug design /synthesis /production; drug metabolism; drug screening /evaluation; prodrugs

The specific objectives of this project are: (a) to synthesize cogeners of synthetic compounds with confirmed activity; (b) to design and synthesize prodrug; (c) to synthesize compounds related to products of natural origin and other related heterocycles; and (d) to synthesize anti-sense nucleic acids. The Contractor shall provide the synthesis effort necessary to advance novel, but flawed, lead anti-AIDS compounds to clinical candidates and for the synthesis of novel compounds based on biochemical/chemical rationale. Often the initially identified lead compounds are flawed because of poor solubility, insufficient stability, and/or narrow spectrum of activity. The "Congener and Prodrug" program will permit the synthesis of clinical anti-AIDS candidate compounds by overcoming these various problems. The quantity of compounds to be synthesized will be dictated by the screening needs.

该项目的具体目标是：（a）合成 具有确认活性的合成化合物的结合体； （b）到 设计和合成前药； （c）合成化合物 与自然来源和其他相关的产品有关 杂环； （d）合成抗义核酸。 承包商应提供必要的综合工作 预付小说，但有缺陷的抗辅助化合物临床上的抗艾滋病化合物 候选人和基于新颖化合物的合成 生化/化学理由。通常是最初确定的铅 化合物由于溶解度差而存在缺陷，不足 稳定性和/或活动范围狭窄。 “同型人和 前药程序将允许合成临床抗AID 候选化合物通过克服这些各种问题。 这 要合成的化合物的数量将由 筛选需求。