COMBINATORIAL APPROACHES TO ANTI-SMALLPOX AGENTS

抗天花药物的组合方法

• 批准号: 6655708
• 负责人: MICHAEL C PIRRUNG
• 金额: $ 34.27万
• 依托单位: DUKE UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 2000
• 资助国家: 美国
• 起止时间: 2000-08-15 至 2005-06-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6655708
• 关键词: Poxviridae; antiviral agents; biotechnology; bioterrorism /chemical warfare; combinatorial chemistry; cooperative study; drug design /synthesis /production; high throughput technology

DESCRIPTION (adapted from the application): The long-term goal of this research is to develop novel anti-biological threat agents using combinatorial methods. The specific objectives of this program are the development of novel anti-smallpox agents. The main projects involve: preparation of libraries of drug-like molecules by high-throughput, parallel synthesis methods, and combinatorial biosynthesis for testing in high-throughput screens. The targets include vaccinia topoisomerase and H1-phosphatase. This project will utilize the following methods: (1) organic synthesis, both in solution and on the solid phase, and combinatorial chemistry; (2) microbial molecular genetics, combinatorial biosynthesis and natural product fermentation; and (3) viral molecular genetics, heterologous protein expression, in vitro enzyme assays, and antiviral assays in tissue culture.

描述（根据应用程序改编）：这是此的长期目标 研究是使用组合制定新颖的抗生物威胁剂 方法。 该计划的具体目标是新颖的发展 抗Smallpox药物。 主要项目涉及：准备图书馆 通过高通量，平行合成方法的药物样分子和 用于在高通量屏幕中测试的组合生物合成。 这 靶标包括牛t型拓扑异构酶和H1-磷酸酶。 该项目将利用以下方法：（1）有机综合，两者都 在溶液和固相和组合化学中； （2）微生物 分子遗传学，联合生物合成和天然产物 发酵； （3）病毒分子遗传学，异源蛋白 在组织培养中表达，体外酶测定和抗病毒测定。

项目成果

Inhibition of Cdc25 phosphatases by indolyldihydroxyquinones.

• DOI: 10.1021/jm0300835
• 发表时间: 2003-05
• 期刊: Journal of medicinal chemistry
• 影响因子: 7.3
• 作者: J. Sohn;B. Kiburz;Zhitao Li;Liu Deng;Alexias Safi;M. Pirrung;J. Rudolph

Modular, parallel synthesis of an illudinoid combinatorial library.

• DOI: 10.1021/ol034565m
• 发表时间: 2003-04
• 期刊: Organic letters
• 影响因子: 5.2
• 作者: M. Pirrung;Hao Liu