REACTOR FOR GENERATION OF COMPOUND DERIVATIVE LIBRARIES

用于生成化合物衍生库的反应器

• 批准号: 2024050
• 负责人: James B. West
• 金额: $ 10万
• 依托单位: BEND RESEARCH, INC.
• 依托单位国家: 美国
• 财政年份: 1997
• 资助国家: 美国
• 起止时间: 1997-06-01 至 1997-11-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/2024050
• 关键词: biomedical equipment development; bioreactors; chemical registry /resource; chemical synthesis; method development; nicotine

DESCRIPTION: (Adapted from the applicant's abstract) The goal of this program is to develop a new process for rapidly generating mixtures of derivatives (i.e., derivative libraries) of compounds with pharmaceutical activity. Such derivatives are made from compounds possessing biological activity or from close analogues of these compounds, with the goal of identifying related compounds with more attractive pharmaceutical properties, such as aqueous solubility, GI-tract permeability, or target selectivity. The proposed process should make it possible to produce structurally distinct derivatives rapidly and to produce derivatives not readily accessible from the parent compound using traditional chemical methods. The process promises to greatly accelerate the optimization and development of pharmaceutical leads. In Phase I, it is planned to demonstrate the feasibility of this process by derivatizing known agonists of three nicotinic acetylcholine receptors - compounds that exhibit interesting neuroprotective activities but have not yet been developed into commercial pharmaceuticals. In Phase II, the process and reactor design would be optimized for rapidly generating derivative libraries from a range of starting materials using a series of derivatizing molecules. Due to the promise of this technology, a major pharmaceutical company has agreed to collaborate with Bend Research by screening the derivative libraries for bioactivity for a broad range of therapeutic uses.

描述：(改编自申请者的摘要)这一目标 计划是开发一种快速产生混合物的新工艺 含有药物的化合物的衍生物(即衍生物库) 活动。这种衍生品是由具有生物特性的化合物制成的。 活性或来自这些化合物的密切类似物，目标是 用更具吸引力的药物鉴定相关化合物 性质，如水的溶解度、胃肠道渗透性或靶标 选择性。 拟议的工艺应使其能够在结构上生产 不同的衍生品迅速和不容易地产生衍生品 使用传统的化学方法从母体化合物中获得。 这一过程有望极大地加快优化和 开发药物先导。 在第一阶段，计划论证这一进程的可行性。 通过衍生已知的三种烟碱型乙酰胆碱受体激动剂 -表现出有趣的神经保护活性但具有 还没有开发成商业药品。 在第二阶段，将对工艺和反应堆设计进行快速优化 使用从一系列起始材料生成衍生库 一系列衍生分子。由于这一承诺 科技，一家大型制药公司已同意与 通过筛选具有生物活性的衍生库进行弯曲研究 广泛的治疗用途。