Liquid Chromatography System with Mass-Based Analysis and Purification to Support Departmental Reaction Optimization and Medicinal Chemistry Programs

具有基于质量的分析和纯化功能的液相色谱系统,支持部门反应优化和药物化学项目

基本信息

  • 批准号:
    RTI-2020-00115
  • 负责人:
  • 金额:
    $ 10.93万
  • 依托单位:
  • 依托单位国家:
    加拿大
  • 项目类别:
    Research Tools and Instruments
  • 财政年份:
    2019
  • 资助国家:
    加拿大
  • 起止时间:
    2019-01-01 至 2020-12-31
  • 项目状态:
    已结题

项目摘要

With discoveries like drugs, insecticides, polymers, and food additives, organic chemistry is a powerful science that has helped our modern society enjoy a dramatic increase in life expectancy and standard of living in the past century. The discovery of new drugs and commodity chemicals rely on a continuous input of new reactions and new compounds to be tested for the desired applications. In the field of drug discovery, numerous compounds must be designed, synthesized, purified and tested iteratively until an optimal molecules is identified that possesses all of the desired beneficial properties. Research laboratories of both co-applicants are actively involved in a number of focused drug discovery projects with collaborators in the Faculty of Medicine, as well as other early-stage projects aimed at developing new chemotypes and new methods to produce small molecules of medicinal interest. The technology of high-performance liquid chromatography coupled with mass spectrometric detection (LCMS) with mass-based purification is essential in various stages of these projects, for example to purify small amounts of compounds for biological testing, to perform pre- or post-assay quality control, or even to assess the stability of lead compounds under different media and storage conditions. Our current departmental LCMS instrument is a workhorse system, purchased in 2004, that is often utilized day and night (with programmed injections) for an average of 30 hours/week. This system is several generations behind current models, and is no longer supported by the vendor. It is deteriorating rapidly, which jeopardizes the progress of numerous drug discovery projects and other activities that rely on this invaluable technology. Thus, this RTI application describes a proposal to acquire a modern HPLC-ESMS system equipped with mass-based analysis and semi-preparative purification to support the daily organic synthesis activities of the co-applicants' laboratories and their numerous medicinal chemistry collaborations, particularly in oncology research. The system will be a key component of a compound purification and analysis service facility within a departmental Analytical and Instrumentation Laboratory, which also supports other programs in the U of A Department of Chemistry. It will support applied medicinal chemistry projects and other synthetic methodology development projects in all aspects of reaction optimization, analysis, and purification. The urgent need for the requested instrument is acutely illustrated by the very recent failure of the autosampler on the current obsolete instrument, which was deemed unserviceable by the original vendor. A new instrument would immediately support and enhance the training environment of over 25 HQP in the research groups of the co-applicants and others. Moreover, it would be managed and maintained, by a full-time, highly experience technologist within a dedicated departmental facility.
随着药物,杀虫剂,聚合物和食品添加剂的发现,有机化学是一门强大的科学,帮助我们的现代社会在过去的世纪中大幅提高了预期寿命和生活水平。新药和日用化学品的发现依赖于新反应和新化合物的持续输入,以测试所需的应用。在药物发现领域,必须反复设计、合成、纯化和测试许多化合物,直到鉴定出具有所有期望的有益特性的最佳分子。两个共同申请人的研究实验室都积极参与了一些集中的药物发现项目与合作者在医学院,以及其他早期项目,旨在开发新的化学型和新方法,以生产小分子的药用利益。在这些项目的各个阶段,高效液相色谱与质谱检测(LCMS)相结合的技术以及基于质量的纯化是必不可少的,例如纯化少量化合物用于生物测试,进行分析前或分析后的质量控制,甚至评估先导化合物在不同介质和储存条件下的稳定性。我们目前的部门LCMS仪器是一个主力系统,购买于2004年,这是经常利用日夜(与编程注射)平均30小时/周。该系统比当前型号落后几代,供应商不再支持该系统。它正在迅速恶化,这危及许多药物发现项目和依赖这一宝贵技术的其他活动的进展。因此,该RTI申请描述了一项获得配备有基于质量的分析和半制备纯化的现代HPLC-ESMS系统的提议,以支持共同申请人实验室的日常有机合成活动及其众多药物化学合作,特别是在肿瘤学研究中。该系统将是一个部门分析和仪器实验室内的化合物纯化和分析服务设施的关键组成部分,该实验室还支持化学系U的其他项目。它将在反应优化、分析和纯化的各个方面支持应用药物化学项目和其他合成方法学开发项目。最近,原供应商认为过时仪器上的自动取样器出现故障,这一点清楚地表明迫切需要所要求的仪器。一个新的工具将立即支持和加强在共同申请人和其他人的研究小组超过25个HQP的培训环境。此外,该系统将由一名经验丰富的全职技术专家在一个专门的部门设施内管理和维护。

项目成果

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Hall, Dennis其他文献

Hall, Dennis的其他文献

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{{ truncateString('Hall, Dennis', 18)}}的其他基金

Boron Chemistry for Catalysis and Drug Discovery
用于催化和药物发现的硼化学
  • 批准号:
    CRC-2015-00074
  • 财政年份:
    2022
  • 资助金额:
    $ 10.93万
  • 项目类别:
    Canada Research Chairs
Boron Chemistry for Catalysis and Drug Discovery
用于催化和药物发现的硼化学
  • 批准号:
    CRC-2021-00419
  • 财政年份:
    2022
  • 资助金额:
    $ 10.93万
  • 项目类别:
    Canada Research Chairs
Boronic Acid Chemistry as a Modern Platform in Catalysis, Stereocontrolled Synthesis and Bioconjugation
硼酸化学作为催化、立体控制合成和生物共轭的现代平台
  • 批准号:
    RGPIN-2017-05086
  • 财政年份:
    2021
  • 资助金额:
    $ 10.93万
  • 项目类别:
    Discovery Grants Program - Individual
Boron Chemistry For Catalysis And Drug Discovery
用于催化和药物发现的硼化学
  • 批准号:
    CRC-2015-00074
  • 财政年份:
    2021
  • 资助金额:
    $ 10.93万
  • 项目类别:
    Canada Research Chairs
Boronic Acid Chemistry as a Modern Platform in Catalysis, Stereocontrolled Synthesis and Bioconjugation
硼酸化学作为催化、立体控制合成和生物共轭的现代平台
  • 批准号:
    RGPIN-2017-05086
  • 财政年份:
    2020
  • 资助金额:
    $ 10.93万
  • 项目类别:
    Discovery Grants Program - Individual
Boron Chemistry for Catalysis and Drug Discovery
用于催化和药物发现的硼化学
  • 批准号:
    CRC-2015-00074
  • 财政年份:
    2020
  • 资助金额:
    $ 10.93万
  • 项目类别:
    Canada Research Chairs
Boronic Acid Chemistry as a Modern Platform in Catalysis, Stereocontrolled Synthesis and Bioconjugation
硼酸化学作为催化、立体控制合成和生物共轭的现代平台
  • 批准号:
    RGPIN-2017-05086
  • 财政年份:
    2019
  • 资助金额:
    $ 10.93万
  • 项目类别:
    Discovery Grants Program - Individual
Boron Chemistry for Catalysis and Drug Discovery
用于催化和药物发现的硼化学
  • 批准号:
    CRC-2015-00074
  • 财政年份:
    2019
  • 资助金额:
    $ 10.93万
  • 项目类别:
    Canada Research Chairs
Boronic Acid Chemistry as a Modern Platform in Catalysis, Stereocontrolled Synthesis and Bioconjugation
硼酸化学作为催化、立体控制合成和生物共轭的现代平台
  • 批准号:
    RGPIN-2017-05086
  • 财政年份:
    2018
  • 资助金额:
    $ 10.93万
  • 项目类别:
    Discovery Grants Program - Individual
Boron Chemistry for Catalysis and Drug Discovery
用于催化和药物发现的硼化学
  • 批准号:
    CRC-2015-00074
  • 财政年份:
    2018
  • 资助金额:
    $ 10.93万
  • 项目类别:
    Canada Research Chairs

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