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: 8361168
• 负责人: BRENT ABRAHAM
• 金额: --
• 依托单位: UNIVERSITY OF WISCONSIN-MADISON
• 依托单位国家: 美国
• 财政年份: 2011
• 资助国家: 美国
• 起止时间: 2011-03-01 至 2012-02-29
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/8361168
• 关键词: Alzheimer' s Disease; Binding; Biochemistry; Biological; Brain; Central Nervous System Diseases; Characteristics; Chemistry; Development; Funding; Grant; Molecular Conformation; Muscarinic Acetylcholine Receptor; Muscarinic Agonists; National Center for Research Resources; Pharmaceutical Chemistry; Pharmaceutical Preparations; Pharmacologic Substance; Principal Investigator; Research; Research Infrastructure; Resources; Schizophrenia; Source; Structure; Structure-Activity Relationship; United States National Institutes of Health; base; cost; 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. Primary support for the subproject and the subproject's principal investigator may have been provided by other sources, including other NIH sources. The Total Cost listed for the subproject likely represents the estimated amount of Center infrastructure utilized by the subproject, not direct funding provided by the NCRR grant to the subproject or subproject staff. 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.

该副本是利用资源的众多研究子项目之一 由NIH/NCRR资助的中心赠款提供。对该子弹的主要支持 而且，副投影的主要研究员可能是其他来源提供的 包括其他NIH来源。 列出的总费用可能 代表subproject使用的中心基础架构的估计量， NCRR赠款不直接向子弹或副本人员提供的直接资金。 Mithridion是一家小分子制药公司，在中枢神经系统疾病（特别是阿尔茨海默氏病和精神分裂症）中进行研究和开发。我们的研究涉及针对与大脑中毒蕈碱受体结合的小分子的结构活性关系（SAR）的药物化学。我们的化学计划需要每天/每周合成许多新化合物。我们合成的化合物必须在组成和结构上充分表征。构象，区域化学和立体化学等结构特征由NMR（1H和13C）确定。通过确定化合物的结构特征以及生物学活性，我们正在探测可用于治疗CNS疾病的潜在药物的结合模式。 UW Madison生物化学的NMR设施对于我们在发现新药以治疗阿尔茨海默氏病和精神分裂症中未满足的需求的研究工作中至关重要。