NEW REACTOR FOR DRUG DISCOVERY LIBRARIES

描述：拟议的第一阶段项目旨在开发一种新的 产生具有独特结构的化合物混合物的方法。AS 可以想象，这些新化合物的混合物(称为化学物质 库“)将具有适当的属性，使它们符合 高通量筛选生物活性以发现 新药。这一过程有望成为一种方便、经济的 一种生产多种结构多样化合物的方法。 在第一阶段，调查人员提议证明新的流程可以 从一系列原料中生产独特化合物的混合物； 2)受到控制，使这种混合物中的大多数化合物 化学和物理性能与大多数 药品：3)适用于高通量生产的高产混合物 筛选；以及4)可重复操作，允许产生 在筛选过程中鉴定出的大量分子 活性(以允许结构阐明)。 在第二阶段，该过程将产生不同种类的化学库 化学成分。一家大型制药公司将合作 与调查人员合作-对化学图书馆进行筛选 广泛用于治疗用途的生物活性。显示的化合物 生物活性将从结构上确定。Active的类似物 将制备化合物，并同样进行生物活性筛选。

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.