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New approaches to antimalarial chemotherapy: design and synthesis of bicyclic endoperoxides and of peptide and peptidomimetic carbonyl containing cysteine protease inhibitors

机译：抗疟疾化学疗法的新方法：双环内过氧化物以及含有半胱氨酸蛋白酶抑制剂的肽和拟肽羰基的设计和合成

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Tese dout., Química Orgânica, Universidade do Algarve, 2007

机译：博士论文，阿尔加威大学有机化学，2007年

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年度 2007
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1. Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. Part 7: structure-activity studies of bicyclic 2-pyridone-containing peptidomimetics. [J] . Dragovich PeterS, Prins ThomasJ, Zhou Ru, Bioorganic and Medicinal Chemistry Letters . 2002,第5期

机译：基于结构的设计，合成和不可逆转的人类鼻病毒3C蛋白酶抑制剂的生物学评估。第7部分：含双环2-吡啶酮的拟肽的结构活性研究。
2. Novel peptidomimetic cysteine protease inhibitors as potential antimalarial agents [J] . Micale N, Kozikowski AP, Ettari R, Journal of Medicinal Chemistry . 2006,第11期

机译：新型拟肽半胱氨酸蛋白酶抑制剂作为潜在的抗疟药
3. Sustainable Synthesis of Novel Arylamide L-Cysteine Methyl Esters Peptidomimetic Derivatives: Inhibitors of Serine and Cysteine-like Proteases [J] . Reis Adriana Karla Cardoso Amorim, Serralbo Aline Silveira, Santos Daniel de Carvalho, Orbital : the Electronic Journal of Chemistry . 2020,第4期

机译：新型芳基酰胺L-半胱氨酸甲酯的可持续合成肽瘤衍生物：丝氨酸和半胱氨酸样蛋白酶的抑制剂
4. Design, Synthesis and Structure of Peptidomimetic Inhibitors of Eukaryotic Ribonucleotide Reductase: A Target for Cancer Chemotherapy [C] . Jaskiran Kaur, Shalini Jha, Chris Dealwis American Peptide Symposium . 2009

机译：真核核糖核苷酸还原酶肽抑制剂的设计，合成和结构：癌症化疗靶标
5. Design, synthesis, and evaluation of novel thiobenzyl ester substrates and aza -peptide inhibitors for serine and cysteine proteases [D] . Rukamp, Brian John 2003

机译：设计，合成和评估新型硫代苄基酯底物和丝氨酸和半胱氨酸蛋白酶的氮杂肽抑制剂
6. Design synthesis and crystallographic analysis of nitrile-based broad-spectrum peptidomimetic inhibitors for coronavirus 3C-like proteases [O] . Chi-Pang Chuck, Chao Chen, Zhihai Ke, -1

机译：冠状病毒3C样蛋白酶的腈基广谱拟肽抑制剂的设计合成和晶体学分析
7. Metabotropic glutamate receptor 3 neuroprotection A. Berent-Spillson and J. W. Russell Received June 12, 2006; revised manuscript received October 3, 2006; accepted October 5, 2006. Address correspondence and reprint requests to James W. Russell, Department of Neurology, University of Maryland School of Medicine, 22 South Greene Street, Baltimore, MD 21201-1595, USA. E-mail: jruss@umich.edu Abbreviations used : APDC , 2 R ,4 R -4-aminopyrrolidine-2,4-dicarboxylate (specific metabotropic glutamate receptor 3 agonist) ; BSO , buthionine sulfoximine (GSH synthesis inhibitor) ; caspase , cysteine-requiring aspartate protease ; CysGly , cysteinylglycine (GSH degradation product) ; DAPI , 4′-6-diamidino-2-phenylindole ; DCF , dichlorodihydrofluorescein ; DCFDA , 5-(and 6)-chloromethyl-2′,7′-dichlorodihydrofluorescein diacetate, acetyl ester ; DHE , dihydroethidium ; DRG , dorsal root ganglion ; FCCP , carbonyl cyanide 4-(trifluoromethoxy)phenylhydrazone (electron transport uncoupler) ; GCP II/III , glutamate carboxypeptidase II/III ; GSH , glutathione ; GSH-EE , glutathione ethyl ester ; GST , glutathione-s-transferase ; H 2 O 2 , hydrogen peroxide ; HBSS , Hank’s balanced salt solution ; JC-1 , 5,5′,6,6′-tetrachloro-1,1′,3,3′-tetraethylbenzimidazolylcarbocyanine iodide ; MCB , monochlorobimane ; mGluR , metabotropic glutamate receptor ; NAAG , N -acetyl-aspartyl-glutamate ; PBS , phosphate-buffered saline ; PCD , programmed cell death ; Rh123 , rhodamine123 ; ROS , reactive oxygen species ; δψ μ , inner mitochondrial membrane potential . Metabotropic glutamate receptor 3 protects neurons from glucose-induced oxidative injury by increasing intracellular glutathione concentration [O] . Berent-Spillson Alison, Russell James W. 2007

机译：代谢型谷氨酸受体3神经保护a. Berent-spillson和J. W. Russell于2006年6月12日收到;修订稿于2006年10月3日收到; 2006年10月5日接受。美国马里兰州巴尔的摩市南格林街22号，马里兰大学医学院神经病学系James W. Russell的地址通信和重印申请。电子邮件：jruss@umich.edu使用的缩写：apDC，2R，4R-4-氨基吡咯烷-2,4-二羧酸酯（特异性代谢型谷氨酸受体3激动剂）; BsO，丁硫氨酸亚砜亚胺（GsH合成抑制剂）;半胱天冬酶，半胱氨酸需要的天冬氨酸蛋白酶; CysGly，半胱氨酰甘氨酸（GsH降解产物）; DapI，4'-6-二脒基-2-苯基吲哚; DCF，二氯二氢荧光素; DCFDa，5-（和6） - 氯甲基-2'，7'-二氯二氢荧光素二乙酸酯，乙酰酯; DHE，二氢乙锭; DRG，背根神经节; FCCp，羰基氰化物4-（三氟甲氧基）苯腙（电子传输解偶联剂）; GCp II / III，谷氨酸羧肽酶II / III;谷胱甘肽;谷胱甘肽; GsH-EE，谷胱甘肽乙酯; GsT，谷胱甘肽-s-转移酶; H 2 O 2，过氧化氢; HBss，Hank的平衡盐溶液; JC-1,5,5'，6,6'-四氯-1,1'，3,3'-四乙基苯并咪唑基酞菁碘化物; mCB，monochlorobimane; mGluR，代谢型谷氨酸受体; NaaG，N-乙酰基 - 天冬氨酰谷氨酸; pBs，磷酸盐缓冲盐水; pCD，程序性细胞死亡; Rh123，罗丹明123;活性氧，活性氧; δψμ，线粒体内膜电位。代谢型谷氨酸受体3通过增加细胞内谷胱甘肽浓度来保护神经元免受葡萄糖诱导的氧化损伤

New approaches to antimalarial chemotherapy: design and synthesis of bicyclic endoperoxides and of peptide and peptidomimetic carbonyl containing cysteine protease inhibitors

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