NEW REACTOR FOR DRUG DISCOVERY LIBRARIES

用于药物发现库的新反应器

• 批准号: 2771058
• 负责人: James B. West
• 金额: $ 36.64万
• 依托单位: BEND RESEARCH, INC.
• 依托单位国家: 美国
• 财政年份: 1996
• 资助国家: 美国
• 起止时间: 1996-06-01 至 1999-08-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/2771058
• 关键词: biomedical equipment development; bioreactors; chemical registry /resource; chemical structure; drug design /synthesis /production; drug screening /evaluation; method development

DESCRIPTION: The proposed Phase I project is aimed at developing a new process for generating mixtures of compounds with unique structures. As envisioned, these mixtures of novel compounds (termed "chemical libraries") will have attributes appropriate for subjecting them to high-throughput screening of bioactivity for the purpose of discovering new pharmaceuticals. The process promises to be a convenient, economical method for producing many structurally diverse compounds. In Phase I the investigators propose to show that the new process can 1) produce mixtures of unique compounds from a range of starting materials; 2) be controlled so that the majority of compounds in this mixture have chemical and physical properties that match those of most pharmaceuticals: 3) yield mixtures suitable for use in high-throughput screening; and 4) operate reproducibly, allowing generation of substantial quantities of molecules identified during screening as active (to allow structure elucidation). In Phase II the process will generate chemical libraries with diverse chemical compositions. A major pharmaceutical company will collaborate with the investigators - subjecting the chemical libraries to screening of bioactivity for a broad range of therapeutic uses. Compounds shown to be bioactive will be structurally identified. Analogs of active compounds will be prepared and likewise screened for bioactivity.

描述：拟议的第一阶段项目旨在开发一种新的 制备具有独特结构的化合物的混合物的方法。 作为 可以预见，这些新化合物的混合物（称为“化学混合物”） 库”）将具有适合于使它们服从 高通量筛选生物活性以发现 新药 该过程有望成为一种方便，经济 生产许多结构不同的化合物的方法。 在第一阶段，研究人员提出，新的过程可以1） 从一系列起始材料中生产独特化合物的混合物; 2)应加以控制，使该混合物中的大多数化合物 化学和物理性质与大多数 药物：3）产生适合用于高通量的混合物 筛选;和4）可重复地操作，允许产生 在筛选期间鉴定的大量分子， 活性（允许结构解析）。 在第二阶段，该过程将产生具有不同化学性质的化学库。 化学成分 一家大型制药公司将与 与研究人员一起-对化学文库进行筛选 具有广泛的治疗用途。 示化合物 将在结构上被鉴定为具有生物活性。 活性类似物 将制备化合物并同样筛选其生物活性。