Synthesis of spiro-1,2-dioxolanes and their activity against Plasmodium falciparum.

Martyn DC; Ramirez AP; Beattie MJ; Cortese JF; Patel V; Rush MA; Woerpel KA; Clardy J

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Synthesis of spiro-1,2-dioxolanes and their activity against Plasmodium falciparum.

机译：螺1,2-二氧戊环的合成及其对恶性疟原虫的活性。

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Artemisinin-derived compounds play an integral role in current malaria chemotherapy. Given the virtual certainty of emerging resistance, we have investigated spiro-1,2-dioxolanes as an alternative scaffold. The endoperoxide functionality was generated by the SnCl(4)-mediated annulation of a bis-silylperoxide and an alkene. The first set of eight analogs gave EC(50) values of 50-150 nM against Plasmodium falciparum 3D7 and Dd2 strains, except for the carboxylic acid analog. A second series, synthesized by coupling a spiro-1,2-dioxolane carboxylic acid to four separate amines, afforded the most potent compound (EC(50) approximately 5 nM).

机译：青蒿素衍生的化合物在当前的疟疾化疗中起着不可或缺的作用。鉴于新出现的耐药性的确定性，我们已经研究了螺1,2-二氧戊环作为替代支架。内过氧化物官能度是由Sn-Cl（4）介导的双甲硅烷基过氧化物和烯烃的环化反应生成的。第一组八个类似物针对恶性疟原虫3D7和Dd2菌株的EC（50）值为50-150 nM，但羧酸类似物除外。通过将螺-1,2-二氧戊环羧酸与四个单独的胺偶联而合成的第二个系列提供了最有效的化合物（EC（50）约为5 nM）。

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《Bioorganic and Medicinal Chemistry Letters》 |2008年第24期|共4页
作者
Martyn DC; Ramirez AP; Beattie MJ; Cortese JF; Patel V; Rush MA; Woerpel KA; Clardy J;
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正文语种 eng
中图分类药学;生物化学;
关键词
Plasmodium falciparum; Synthesis; Nanomole/liter; analogs; Carboxylic Acids; 疟原虫; 恶性; 羧酸类;

机译：Plasmodium falciparum;Synthesis;Nanomole/liter;analogs;Carboxylic Acids;疟原虫;恶性;羧酸类;

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1. Synthesis of spiro-1,2-dioxolanes and their activity against Plasmodium falciparum. [J] . Martyn DC, Ramirez AP, Beattie MJ, Bioorganic and Medicinal Chemistry Letters . 2008,第24期

机译：螺1,2-二氧戊环的合成及其对恶性疟原虫的活性。
2. Synthesis and in vitro DMPK profiling of a 1,2-dioxolane-based library with activity against Plasmodium falciparum. [J] . Martyn DC, Beletsky G, Cortese JF Bioorganic and Medicinal Chemistry Letters . 2009,第19期

机译：具有对恶性疟原虫活性的基于1,2-二氧戊环的文库的合成和体外DMPK分析。
3. Synthesis and in vitro activities of ferrocenic aminohydroxynaphthoquinones against Toxoplasma gondii and Plasmodium falciparum. [J] . Baramee A, Coppin A, Mortuaire M, Bioorganic and medicinal chemistry . 2006,第5期

机译：二茂铁氨基羟基萘醌的合成及其体外抗弓形虫和恶性疟原虫的活性。
4. In vitro antiplasmodial activity of extract and fraction of temu mangga (Curcuma mangga) against Plasmodium falciparum 3D7 [C] . Dhina Fitriastuti, Annisa Wahyu Nur Iman, Dea Alvine Lutfiani, International Conference on Chemistry, Chemical Process and Engineering . 2018

机译：对疟原虫疟原虫（Curcuma Mangga）提取物和分数的体外抗蛋乳活性对抗疟原虫3D7
5. Genetic exploration of the ATP synthase complex in Plasmodium falciparum. [D] . Pershing, April M. 2016

机译：恶性疟原虫中ATP合酶复合物的遗传探索。
6. Biosynthesis, export and processing of a 45 kDa protein detected in membrane clefts of erythrocytes infected with Plasmodium falciparum. [O] . A Das, H G Elmendorf, W I Li, 2018

机译：在恶性疟原虫感染的红细胞膜裂中检测到的45 kDa蛋白的生物合成，输出和加工。
7. Synthesis of New 4-Aminoquinolines and Evaluation of Their In Vitro Activity against Chloroquine-Sensitive and Chloroquine-Resistant Plasmodium falciparum. [O] . Chandima S K Rajapakse, Maryna Lisai, Christiane Deregnaucourt, 2015

机译：新型4-氨基喹啉的合成及其对氯喹敏感和氯喹抗性恶性疟原虫的体外活性评价。
8. Comparison of the In Vitro Activities of Admodiaquine and Desethylamodiaquine against Isolates of Plasmodium falciparum. (Reannouncement with New Availability Information). [R] . Childs, G. E., Boudreau, E. F., Milhous, W. K., 1989

机译：admodiaquine和Desethylamodiaquine对恶性疟原虫分离株的体外活性比较。（重新公布新的可用性信息）。

Synthesis of spiro-1,2-dioxolanes and their activity against Plasmodium falciparum.

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