Design and synthesis of new antimalarial agents from 4-aminoquinoline.

Solomon VR; Puri SK; Srivastava K; Katti SB

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Design and synthesis of new antimalarial agents from 4-aminoquinoline.

机译：从4-氨基喹啉设计和合成新型抗疟药。

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摘要

This study describes the synthesis of new 4-aminoquinoline derivatives and evaluation of their activity against a chloroquine sensitive strain of P. falciparum in vitro and chloroquine resistant N-67 strain of P. yoelii in vivo. All the analogues were found to form strong complex with hematin and inhibit the beta-hematin formation in vitro. These results suggest that these compounds act on heme polymerization target.

机译：这项研究描述了新的4-氨基喹啉衍生物的合成及其在体外对恶性疟原虫对氯喹敏感菌株和体内对耐氯喹的约氏疟原虫N-67菌株的活性评估。发现所有类似物与血红素形成强复合物并在体外抑制β-血红素的形成。这些结果表明这些化合物对血红素聚合目标起作用。

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来源
《Bioorganic and Medicinal Chemistry》 |2005年第6期|P.2157-2165|共9页
作者
Solomon VR; Puri SK; Srivastava K; Katti SB;
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作者单位

Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow 226 001, India.;

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原文格式 PDF
正文语种 eng
中图分类基础医学;
关键词
4-aminoquinoline; In Vitro; Chloroquine; 氯喹;

机译：4-氨基喹啉;体外;氯喹;氯喹;

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1. Synthesis and antimalarial activity of novel side chain modified antimalarial agents derived from 4-aminoquinoline. [J] . Solomon VR, Haq W, Smilkstein M, Medicinal chemistry . 2008,第5期

机译：衍生自4-氨基喹啉的新型侧链修饰抗疟剂的合成及其抗疟活性。
2. New Potential Antimalarial Agents: Design, Synthesis and Biological Evaluation of Some Novel Quinoline Derivatives as Antimalarial Agents [J] . Radini Ibrahim Ali M., Elsheikh Tarek M. Y., El-Telbani Emad M., Molecules . 2016,第7期

机译：新的潜在抗疟药：一些新颖的喹啉衍生物作为抗疟药的设计，合成和生物学评估
3. New Potential Antimalarial Agents: Design, Synthesis and Biological Evaluation of Some Novel Quinoline Derivatives as Antimalarial Agents [J] . Ibrahim Radini, Tarek Elsheikh, Emad El-Telbani, Molecules . 2016,第7期

机译：新的潜在抗疟药：一些新颖的喹啉衍生物作为抗疟药的设计，合成和生物学评估
4. In Silico Three Dimensional Pharmacophore Models to Aid the Discovery and Design of New Antimalarial Agents [C] . Apurba K. Bhattacharjee, Mark G. Hartell, Daniel A. Nichols, International Conference on Computational Science(ICCS 2006) pt.1; 20060528-31; Reading(GB) . 2006

机译：In Silico三维药理学模型可帮助发现和设计新的抗疟药
5. Studies in synthetic organic chemistry: Part I. The synthesis of novel antimalarial artmeisinin dimers. Part II. Electronically stabilized versions of antimalarial acetal trioxanes. Part III. Novel analogs of natural hormone 1-alpha, 25-dihdroxyvitamin D3: Design, synthesis and biological evaluation of CYP24 inhibitors. Part IV. New silicon mediated ring expansions of N-sized 2-cycloalkenones into homoallylic N+3 sized lactones. [D] . Kalinda, Alvin Solomon. 2009

机译：合成有机化学研究：第一部分。新型抗疟药青蒿素二聚体的合成。第二部分电子稳定版的抗疟缩醛三恶烷。第三部分天然激素1-α，25-二羟维生素D3的新型类似物：CYP24抑制剂的设计，合成和生物学评估。第四部分新的硅介导的N尺寸的2-环烯酮的环扩环成均烯丙基N + 3尺寸的内酯。
6. New Potential Antimalarial Agents: Design Synthesis and Biological Evaluation of Some Novel Quinoline Derivatives as Antimalarial Agents [O] . Ibrahim Ali M. Radini, Tarek M. Y. Elsheikh, Emad M. El-Telbani, 2016

机译：新的潜在抗疟药：一些新型喹啉衍生物作为抗疟药的设计合成和生物学评估
7. New Potential Antimalarial Agents: Design, Synthesis and Biological Evaluation of Some Novel Quinoline Derivatives as Antimalarial Agents [O] . Ibrahim Ali M. Radini, Tarek M. Y. Elsheikh, Emad M. El-Telbani, 2016

机译：新型潜在抗疟剂：一些新型喹啉衍生物作为抗疟药的设计，合成和生物学评价

Design and synthesis of new antimalarial agents from 4-aminoquinoline.

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