CORE--SYNTHETIC CHEMISTRY AND ANALYTICAL SERVICES

核心--合成化学和分析服务

• 批准号: 6269713
• 负责人: Alexander L Weis
• 金额: $ 9.58万
• 依托单位: UNIVERSITY OF TEXAS HLTH SCIENCE CENTER
• 依托单位国家: 美国
• 财政年份: 1998
• 资助国家: 美国
• 起止时间: 1998-09-30 至 1999-09-29
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6269713
• 关键词: analytical chemistry; biomedical facility; chemical synthesis; cooperative study; drug design /synthesis /production; nucleosides; nucleotides; oligonucleotides; reverse transcriptase inhibitors

The primary role of the chemistry department at the CTRC Research Foundation is the synthesis and analysis of new chemotherapeutic analogs for in vitro and in vivo evaluation. The chemistry laboratories have all of the personnel, equipment and facilities necessary to fulfill the requirements of this core. The Chemistry Core will synthesize compounds including oligonucleotides, nucleosides/nucleotides, and non-nucleoside reverse transcriptase inhibitors to determine structure-activity relationships for Program 1. The Chemistry Core will also support oligonucleotides for Program 2 for footprinting studies; synthesis of specific oligonucleotides for Program 3 for probes for screening of clones; and production of compounds (small scale-up) for in vivo testing carried out in Program 4. Our general approach will be, first, to identify the most efficient synthetic route to the target compound using the synthetic knowledge of the chemistry staff and by searching the literature for known reactions which achieve the chemical transformations needed in the synthesis of the target. Our staff is trained in the use of on-line searching of STN International electronic databases such as Chemical Abstracts, Beilstein, and CAS REACT. Next, a time table will be drawn to assure that the compound can be prepared and characterized by the date required by the program leader. The synthetic route will be approved by the Core Leader and assigned to a synthetic chemist. The progress of the synthesis will be monitored weekly to insure progress is being made. Intermediates and final product will be fully characterized and purity determined using the analytical instrumentation located in-house and described in the analytical section. Strict guidelines will be adhered to in the quality of product prepared for the NCDDG. Final product will be submitted to the Program Leader with a written report indicating the synthetic route followed and the analytical data generated to characterize the compound and determine its purity.

化学系在CTRC研究中的主要作用 基础是新的化疗药物类似物的合成和分析 用于体外和体内评价。化学实验室都有 履行《公约》所需的人员、设备和设施 这个核心的要求。 化学核心将合成包括寡核苷酸在内的化合物， 核苷/核苷酸和非核苷逆转录酶 抑制剂，以确定程序1的结构-活性关系。 化学核心还将支持计划2的寡核苷酸， 足迹法研究;用于程序的特异性寡核苷酸的合成 3用于筛选克隆的探针;和化合物的生产（小 放大）用于程序4中进行的体内测试。 我们的一般做法是，首先，确定最有效的 使用以下合成知识合成目标化合物的合成路线： 化学工作人员和通过搜索已知反应的文献 其实现了合成所述化合物所需的化学转化， 目标我们的员工都受过使用网上搜寻资料的训练。 国际电子数据库，如化学文摘，贝尔斯坦， CAS反应。接下来，将绘制一个时间表，以确保 化合物可以通过本发明要求的日期制备和表征。 项目负责人。合成路线将由核心负责人批准 并被分配给一位合成化学家综合的进展将是 每周进行监测，以确保取得进展。中间体和最终 产品将进行充分表征，并使用 分析仪器位于内部，并在 分析部分。在质量方面将坚持严格的准则， 为NCDDG准备的产品。最终产品将提交给 项目负责人提供指示合成路线的书面报告 随后，生成分析数据以表征化合物 并确定其纯度。