UCD Combinatorial Center - Novel and Diverse Pilot-Scale Library Production (RMI)
UCD 组合中心 - 新颖且多样化的中试规模文库生产 (RMI)
基本信息
- 批准号:7269304
- 负责人:
- 金额:$ 45.4万
- 依托单位:
- 依托单位国家:美国
- 项目类别:
- 财政年份:2005
- 资助国家:美国
- 起止时间:2005-09-23 至 2009-07-31
- 项目状态:已结题
- 来源:
- 关键词:ArchivesBindingBiochemicalBiological AssayCellsChemicalsChemistryChromatographyCouplingDevelopmentDinitrobenzenesEndopeptidasesEnzymesEvaluationGenerationsHigh Pressure Liquid ChromatographyInternetLaboratoriesLibrariesLinkMass Spectrum AnalysisMethodologyMethodsMicroarray AnalysisNumbersOutputPeptide HydrolasesPhasePhosphorylationPhosphotransferasesProceduresProductionPublishingQuality ControlRouteS PhaseSiteSolidSolutionsSystemTestingUnited States National Institutes of Healthbasecombinatorialcombinatorial chemistrydesignexperiencefunctional groupmembernovelresponsescaffoldsmall moleculesolid solution
项目摘要
DESCRIPTION (provided by applicant): In response to the RFA-RM-05-014, we plan to use both solid- and solution-phase strategies to synthesize several pilot-scale libraries to be submitted to NIH for subsequent distribution for various biological assays. Our aim is to prepare chemically pure, structurally diverse small-molecule compounds. These small-molecule compounds will be prepared by adaptation of published synthetic routes or, as appropriate, by development of novel synthetic strategies. Diversity-oriented synthesis (DOS) libraries will generally have ~100-200 members each with =90% purity of non-commercial small-molecules. Our plan is to prepare two types of libraries for each scaffold: (i) a small demo library to test the chemistry and validate the procedures, using the IRORI system for compound synthesis and tracking; (ii) a Trident- or IRORI-based library to deliver a focused library of compounds. The output of libraries (i) and (ii) will be combined, archived, and made available for biochemical evaluation. The dinitrodifluorobenzene-based scaffold will be prepared in larger number and quantity. Some of the solid-phase synthesis libraries will be generated with a built-in hydrophilic handle with site-specific functional groups so that these compounds can be subsequently tagged for specific assays while others will be prepared without any handle. Each compound will be analyzed by HPLC for purity and its identity confirmed by mass spectroscopy. If needed, FlashTube advanced flash chromatography will be used for compound purification. The NIH PubChem will be used for management of our various pilot libraries and we plan to set up a UC Davis Combinatorial Chemistry web site with links to PubChem. As required by the RFA, at least 10 mg of each library member will be archived and each will have =90% purity.
描述(由申请人提供):作为对RFA-RM-05-014的回应,我们计划使用固相和液相策略合成几个中试规模文库,以提交给NIH,用于随后的各种生物测定。我们的目标是制备化学纯,结构多样的小分子化合物。这些小分子化合物将通过改编已发表的合成路线或酌情开发新的合成策略来制备。多样性导向合成(DOS)文库通常具有约100-200个成员,每个成员具有=90%纯度的非商业小分子。我们的计划是为每个支架准备两种类型的库:(i)一个小型演示库,用于测试化学和验证程序,使用IRORI系统进行化合物合成和跟踪;(ii)基于Trident或IRORI的库,用于提供重点化合物库。文库(i)和(ii)的输出将合并、存档并可用于生化评价。基于二硝基二氟苯的支架将被大量制备。一些固相合成文库将用具有位点特异性官能团的内置亲水手柄生成,使得这些化合物可以随后被标记用于特定测定,而其他化合物将在没有任何手柄的情况下制备。将通过HPLC分析各化合物的纯度,并通过质谱法确认其鉴别。如果需要,将使用FlashTube高级快速色谱法进行化合物纯化。美国国立卫生研究院PubChem将用于管理我们的各种试点图书馆,我们计划建立一个加州大学戴维斯分校组合化学网站与PubChem的链接。根据RFA的要求,将至少存档10 mg的每个文库成员,并且每个成员的纯度≥ 90%。
项目成果
期刊论文数量(12)
专著数量(0)
科研奖励数量(0)
会议论文数量(0)
专利数量(0)
Synthesis and biological activity of 2-(4,5-dihydroisoxazol-5-yl)-1,3,4-oxadiazoles.
- DOI:10.1016/j.bmcl.2009.07.139
- 发表时间:2009-10
- 期刊:
- 影响因子:2.7
- 作者:Kristin A. Milinkevich;C. Yoo;T. C. Sparks;B. Lorsbach;M. Kurth
- 通讯作者:Kristin A. Milinkevich;C. Yoo;T. C. Sparks;B. Lorsbach;M. Kurth
3-(Arylthiomethyl)isoxazole-4,5-dicarboxamides: chemoselective nucleophilic chemistry and insecticidal activity.
- DOI:10.1021/jf901512t
- 发表时间:2009-08-26
- 期刊:
- 影响因子:6.1
- 作者:Yu GJ;Iwamoto S;Robins LI;Fettinger JC;Sparks TC;Lorsbach BA;Kurth MJ
- 通讯作者:Kurth MJ
Intramolecular cycloaddition of azomethine ylides in the preparation of pyrrolidino[2',3':3,4]pyrrolidino[1,2- a]benzimidazoles.
偶氮甲碱叶立德在制备吡咯烷[2,3:3,4]吡咯烷[1,2-a]苯并咪唑中的分子内环加成。
- DOI:10.1021/ol702301n
- 发表时间:2007
- 期刊:
- 影响因子:5.2
- 作者:Meng,Liping;Fettinger,JamesC;Kurth,MarkJ
- 通讯作者:Kurth,MarkJ
Synthesis of 5-(thiazol-5-yl)-4,5-dihydroisoxazoles from 3-chloropentane-2,4-dione.
从 3-氯戊烷-2,4-二酮合成 5-(噻唑-5-基)-4,5-二氢异恶唑。
- DOI:10.1021/cc800033m
- 发表时间:2008
- 期刊:
- 影响因子:0
- 作者:Milinkevich,KristinA;Ye,Long;Kurth,MarkJ
- 通讯作者:Kurth,MarkJ
Controlling Selectivity for Cycloadditions of Nitrones and Alkenes Tethered by Benzimidazoles: Combining Experiment and Theory.
- DOI:10.1002/ejoc.200801211
- 发表时间:2009-04
- 期刊:
- 影响因子:2.8
- 作者:Meng, Liping;Wang, Selina C.;Fettinger, James C.;Kurth, Mark J.;Tantillo, Dean J.
- 通讯作者:Tantillo, Dean J.
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MARK J. KURTH其他文献
MARK J. KURTH的其他文献
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{{ truncateString('MARK J. KURTH', 18)}}的其他基金
Complex Heterocycles and Hybrid Strategies for Pilot Scale Libraries
中试规模文库的复杂杂环化合物和混合策略
- 批准号:
8272695 - 财政年份:2010
- 资助金额:
$ 45.4万 - 项目类别:
Complex Heterocycles and Hybrid Strategies for Pilot Scale Libraries
中试规模文库的复杂杂环化合物和混合策略
- 批准号:
7758406 - 财政年份:2010
- 资助金额:
$ 45.4万 - 项目类别:
Complex Heterocycles and Hybrid Strategies for Pilot Scale Libraries
中试规模文库的复杂杂环化合物和混合策略
- 批准号:
8080192 - 财政年份:2010
- 资助金额:
$ 45.4万 - 项目类别:
Novel and Diverse Pilot-Scale Library Production (RMI)
新颖且多样化的中试规模文库生产 (RMI)
- 批准号:
7019300 - 财政年份:2005
- 资助金额:
$ 45.4万 - 项目类别:
UCD Combinatorial Center - Novel and Diverse Pilot-Scal*
UCD 组合中心 - 新颖多样的 Pilot-Scal*
- 批准号:
7125571 - 财政年份:2005
- 资助金额:
$ 45.4万 - 项目类别:
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