DEVELOPMENT AND STUDY OF SMALL MOLECULE MUSCARINIC AGONISTS

小分子毒蕈碱激动剂的开发与研究

• 批准号: 8168971
• 负责人: BRENT ABRAHAM
• 金额: $ 0.01万
• 依托单位: UNIVERSITY OF WISCONSIN-MADISON
• 依托单位国家: 美国
• 财政年份: 2010
• 资助国家: 美国
• 起止时间: 2010-03-01 至 2011-02-28
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/8168971
• 关键词: Alzheimer' s Disease; Binding; Biochemistry; Biological; Brain; Central Nervous System Diseases; Characteristics; Chemistry; Computer Retrieval of Information on Scientific Projects Database; Development; Funding; Grant; Institution; Molecular Conformation; Muscarinic Acetylcholine Receptor; Muscarinic Agonists; Pharmaceutical Chemistry; Pharmaceutical Preparations; Pharmacologic Substance; Research; Research Personnel; Resources; Schizophrenia; Source; Structure; Structure-Activity Relationship; United States National Institutes of Health; base; programs; research and development; small molecule; stereochemistry

This subproject is one of many research subprojects utilizing the resources provided by a Center grant funded by NIH/NCRR. The subproject and investigator (PI) may have received primary funding from another NIH source, and thus could be represented in other CRISP entries. The institution listed is for the Center, which is not necessarily the institution for the investigator. Mithridion is a small molecule pharmaceutical company conducting research and development in central nervous system disorders, specifically Alzheimer's disease and Schizophrenia. Our research involves medicinal chemistry aimed at structure activity relationships (SAR) of small molecules which bind to muscarinic receptors in the brain. Our chemistry program requires the synthesis of many new compounds on a daily/weekly basis. The compounds we synthesize must be fully characterized regarding composition as well as structure. Structural characteristics such as conformation, regiochemistry and stereochemistry, are determined by NMR (both 1H and 13C). By determining structural characteristics of our compounds, as well as biological activity, we are probing the binding modes of potential drugs which may be used to treat CNS diseases. The NMR facility at Biochemistry, UW Madison, is essential for our research efforts in discovering new drugs to treat unmet needs in Alzheimer's disease and Schizophrenia.

该子项目是利用该技术的众多研究子项目之一 资源由 NIH/NCRR 资助的中心拨款提供。子项目和 研究者 (PI) 可能已从 NIH 的另一个来源获得主要资金， 因此可以在其他 CRISP 条目中表示。列出的机构是 对于中心来说，它不一定是研究者的机构。 Mithridion 是一家小分子制药公司，致力于中枢神经系统疾病（特别是阿尔茨海默病和精神分裂症）的研究和开发。我们的研究涉及药物化学，旨在研究与大脑中毒蕈碱受体结合的小分子的结构活性关系（SAR）。我们的化学项目需要每天/每周合成许多新化合物。我们合成的化合物必须充分表征其组成和结构。构象、区域化学和立体化学等结构特征通过 NMR（1H 和 13C）测定。通过确定我们的化合物的结构特征以及生物活性，我们正在探索可用于治疗中枢神经系统疾病的潜在药物的结合模式。威斯康星大学麦迪逊分校生物化学中心的 NMR 设施对于我们发现新药来治疗阿尔茨海默病和精神分裂症未满足的需求的研究工作至关重要。