MEDICINAL CHEMISTRY, CHEMICAL SYNTHESIS, AND MASS SPECTROMETRY
药物化学、化学合成和质谱分析
基本信息
- 批准号:7954019
- 负责人:
- 金额:$ 0.12万
- 依托单位:
- 依托单位国家:美国
- 项目类别:
- 财政年份:2009
- 资助国家:美国
- 起止时间:2009-02-01 至 2010-01-31
- 项目状态:已结题
- 来源:
- 关键词:Acetylcholinesterase InhibitorsAfrica South of the SaharaAlkylationAlzheimer&aposs DiseaseAnopheles gambiaeAreaBenzodiazepinesChemistryComputer Retrieval of Information on Scientific Projects DatabaseCulicidaeFundingGrantInsecticidesInstitutionInterest GroupMalariaMass Spectrum AnalysisMethodsMultinuclear NMRNMR SpectroscopyOrganic SynthesisPathway interactionsPharmaceutical ChemistryReactionReagentResearchResearch PersonnelResourcesRouteSSRI-resistant depressionSourceStructureUnited States National Institutes of HealthWorkbasebeta secretasebeta-site APP cleaving enzyme 1biomedical resourcechemical synthesisinhibitor/antagonistinterestnovelpreventreuptaketransmission process
项目摘要
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.
Medicinal Chemistry. The Carlier group's interests in Medicinal Chemistry encompass three areas. First, they prepare species-selective inhibitors of acetylcholinesterase (AChE) targeting the malaria mosquito (Anopheles gambiae). Such compounds could be deployed on insecticide treated nets to prevent malaria transmission in sub-Saharan Africa. Second, they use click-chemistry based discovery methods to identify BACE1 (beta-secretase) inhibitors; such compounds could be to useful to prevent Alzheimer's disease. Finally, they prepare novel triple reuptake inhibitors to treat SSRI-resistant depression.
Enantioselective Synthetic Methods. Organolithium reagents are ubiquitous in organic synthesis. The Carlier group is interested in developing new stereoselective reactions of organolithium compounds and enolates, and in using computation and multinuclear NMR spectroscopy to determine structures and reaction pathways. Recently they developed an enantioselective alkylation route to a new class of (so-called "quaternary") benzodiazepines. A key feature of this work is the intermediacy of transiently non-racemic ("dynamically chiral") intermediates.
这个子项目是许多研究子项目中的一个
由NIH/NCRR资助的中心赠款提供的资源。子项目和
研究者(PI)可能从另一个NIH来源获得了主要资金,
因此可以在其他CRISP条目中表示。所列机构为
研究中心,而研究中心不一定是研究者所在的机构。
药物化学Carlier集团对药物化学的兴趣包括三个领域。首先,他们制备了针对疟疾蚊子(冈比亚按蚊)的乙酰胆碱酯酶(AChE)物种选择性抑制剂。这种化合物可以用于杀虫剂处理的蚊帐,以防止撒哈拉以南非洲的疟疾传播。其次,他们使用基于点击化学的发现方法来鉴定BACE 1(β-分泌酶)抑制剂;这些化合物可能有助于预防阿尔茨海默病。最后,他们制备了新的三重再摄取抑制剂来治疗SSRI抗性抑郁症。
对映选择性合成方法有机锂试剂在有机合成中普遍存在。Carlier研究组致力于开发有机锂化合物和烯醇化物的新的立体选择性反应,并利用计算和多核NMR光谱来确定结构和反应途径。最近,他们开发了一种对映选择性烷基化路线,以一类新的(所谓的“季”)苯并二氮杂卓。这项工作的一个关键特征是瞬时非外消旋(“动态手性”)中间体的中间性。
项目成果
期刊论文数量(0)
专著数量(0)
科研奖励数量(0)
会议论文数量(0)
专利数量(0)
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Paul R Carlier其他文献
Paul R Carlier的其他文献
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{{ truncateString('Paul R Carlier', 18)}}的其他基金
Optimization of antimalarials targeting multiple life stages of the parasite
针对寄生虫多个生命阶段的抗疟药物的优化
- 批准号:
10745610 - 财政年份:2021
- 资助金额:
$ 0.12万 - 项目类别:
Optimization of antimalarials targeting multiple life stages of the parasite
针对寄生虫多个生命阶段的抗疟药物的优化
- 批准号:
10298005 - 财政年份:2021
- 资助金额:
$ 0.12万 - 项目类别:
Optimization of antimalarials targeting multiple life stages of the parasite
针对寄生虫多个生命阶段的抗疟药物的优化
- 批准号:
10813425 - 财政年份:2021
- 资助金额:
$ 0.12万 - 项目类别:
Optimization of antimalarials targeting multiple life stages of the parasite
针对寄生虫多个生命阶段的抗疟药物的优化
- 批准号:
10689033 - 财政年份:2021
- 资助金额:
$ 0.12万 - 项目类别:
Interrogating plasmodial endocytosis with mefloquine-based affinity probes
用基于甲氟喹的亲和探针检测疟原虫内吞作用
- 批准号:
10089405 - 财政年份:2020
- 资助金额:
$ 0.12万 - 项目类别:
MEDICINAL CHEMISTRY, CHEMICAL SYNTHESIS, AND MASS SPECTROMETRY
药物化学、化学合成和质谱分析
- 批准号:
8168768 - 财政年份:2010
- 资助金额:
$ 0.12万 - 项目类别:
Development of vector-specific, resistance-breaking insecticides to reduce malari
开发病媒特异性、突破耐药性的杀虫剂以减少疟疾
- 批准号:
8237040 - 财政年份:2009
- 资助金额:
$ 0.12万 - 项目类别:
Development of vector-specific, resistance-breaking insecticides to reduce malari
开发病媒特异性、突破耐药性的杀虫剂以减少疟疾
- 批准号:
8445236 - 财政年份:2009
- 资助金额:
$ 0.12万 - 项目类别:
Development of vector-specific, resistance-breaking insecticides to reduce malari
开发针对病媒的抗药性杀虫剂以减少疟疾
- 批准号:
7657602 - 财政年份:2009
- 资助金额:
$ 0.12万 - 项目类别:
Development of vector-specific, resistance-breaking insecticides to reduce malari
开发针对病媒的抗药性杀虫剂以减少疟疾
- 批准号:
7796794 - 财政年份:2009
- 资助金额:
$ 0.12万 - 项目类别:
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