Conformationally Restrained Aromatic Analogues of Fosmidomycin and FR900098.

Kurz T; Schluter K; Pein M; Behrendt C; Bergmann B; Walter RD

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Conformationally Restrained Aromatic Analogues of Fosmidomycin and FR900098.

机译：Fosmidomycin和FR900098的构象约束芳香类似物。

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The synthesis and in-vitro antimalarial activity of conformationally restrained bis(pivaloyloxymethyl) ester analogues of the natural product fosmidomycin is presented. In contrast to alpha-aryl-substituted analogues, conformationally restrained aromatic analogues exhibit only moderate in-vitro antimalarial activity against the chloroquine-sensitive strain 3D7 of Plasmodium falciparum. The most active derivative displays an IC(50) value of 47 muM.

机译：提出了天然产物膦酰胺霉素的构象受限的双（新戊酰氧基甲基）酯类似物的合成和体外抗疟活性。与α-芳基取代的类似物相比，构象受限的芳香族类似物仅对恶性疟原虫的氯喹敏感菌株3D7表现出中等的体外抗疟活性。活性最高的衍生物的IC（50）值为47μM。

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《Archiv der Pharmazie》 |2007年第7期|共6页
作者
Kurz T; Schluter K; Pein M; Behrendt C; Bergmann B; Walter RD;
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正文语种 eng
中图分类药学;
关键词
fosmidomycin; Plasmodium falciparum; Inspiratory Capacity; Esters; Chloroquine; 疟原虫; 恶性; 吸气量; 酯类; 氯喹;

机译：fosmidomycin;Plasmodium falciparum;Inspiratory Capacity;Esters;Chloroquine;疟原虫;恶性;吸气量;酯类;氯喹;

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1. Conformationally Restrained Aromatic Analogues of Fosmidomycin and FR900098. [J] . Kurz T, Schluter K, Pein M, Archiv der Pharmazie . 2007,第7期

机译：Fosmidomycin和FR900098的构象约束芳香类似物。
2. Synthesis and antimalarial activity of chain substituted pivaloyloxymethyl ester analogues of Fosmidomycin and FR900098. [J] . Kurz T, Schluter K, Kaula U, Bioorganic and Medicinal Chemistry . 2006,第15期

机译：磷霉素和FR900098的链取代的新戊酰氧基甲基酯类似物的合成及抗疟活性。
3. Synthesis of alpha-Aryl-Substituted and Conformationally Restricted Fosmidomycin Analogues as Promising Antimalarials [J] . Timothy Haemers, Jochen Wiesner, Roger Busson European journal of organic chemistry . 2006,第17期

机译：合成的α-芳基取代的和构象受限的磷霉素类似物作为有望的抗疟药。
4. Synthesis of oxazinyl analogues of fosmidomycin using RCM methodology [C] . Sarah Van der Jeught, Nicolai Dieltiens, Christian V. Stevens European Symposium on Organic Chemistry . 2009

机译：使用RCM方法合成Fosmidomcycin的恶唑啉基类似物
5. Determination of Conformations of Deoxyribonucleic Acids in Solution by 1H-NMR and Restrained Molecular Dynamics [D] . 片平, 正人 1989

机译：1 H-NMR和约束分子动力学测定溶液中脱氧核糖核酸的构象
6. Inhibition of the Yersinia pestis MethylerythritolPhosphate Pathway of Isoprenoid Biosynthesis byα-Phenyl-Substituted Reverse Fosmidomycin Analogues [O] . Haley S. Ball, Misgina Girma, Mosufa Zainab, 2020

机译：鼠疫耶尔森菌甲基赤藓糖醇的抑制异戊二烯生物合成的磷酸途径α-苯基取代的反向磷霉素类似物
7. Targeting an Aromatic Hotspot in Plasmodium falciparum 1-Deoxy-d-xylulose-5-phosphate Reductoisomerase with -Arylpropyl Analogues of Fosmidomycin [O] . Sooriyaarachchi, Sanjeewani, Chofor, Rene, Risseeuw, Martijn D. P., 2016

机译：靶向与恶草霉素的-芳丙基类似物的恶性疟原虫1-脱氧-d-木酮糖-5-磷酸还原异构酶中的芳香族热点

Conformationally Restrained Aromatic Analogues of Fosmidomycin and FR900098.

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