Bicyclo[2.2.2]octyl esters of dialkylamino acids as antiprotozoals

Christian Schlapper; Werner Seebacher; Marcel Kaiser; Reto Brun; Robert Saf; Robert Weis

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Bicyclo[2.2.2]octyl esters of dialkylamino acids as antiprotozoals

机译：二烷基氨基酸的双环[2.2.2]辛基酯作为抗原生动物

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A couple of bicyclo[2.2.2]octyl esters of 2-dialkylaminoacetic acids were prepared. Their antiplasmodial and ancitry-panosomal activities against Trypanosoma brucei rhodesiense (STIB 900) and the K_1 strain of Plasmodium falciparum (resistant to chloroquine and pyrimethamine) were determined using microplate assays. Structure-activity relationships were discussed. The antiprotozoal activities were remarkably increased by insertion of a second basic centre. The selectivity indices of the most active compounds are superior in the bicyclo-octane series.

机译：制备了2-二烷基氨基乙酸的一对双环[2.2.2]辛基酯。使用微孔板测定法测定了它们对布氏锥虫（STIB 900）和恶性疟原虫K_1菌株（对氯喹和乙胺嘧啶具有抗性）的抗疟原虫和anantry-panosomal活性。讨论了构效关系。通过插入第二个基本中心，抗原生动物活性显着增加。在双环辛烷系列中，最具活性的化合物的选择性指数更高。

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来源
《Bioorganic and Medicinal Chemistry》 |2007年第16期|p.5543-5550|共8页
作者
Christian Schlapper; Werner Seebacher; Marcel Kaiser; Reto Brun; Robert Saf; Robert Weis;
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作者单位

Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, Karl-Franzens-University, Universitaetsplatz 1, A-8010 Graz, Austria;

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原文格式 PDF
正文语种 eng
中图分类药学;生物化学;
关键词
4-aminobicyclo2.2.2octane derivatives; trypanosoma brucei rhodesiense; plasmodium falciparum; amino acids;

机译：4-氨基双环[2.2.2]辛烷衍生物;布氏锥虫;恶性疟原虫;氨基酸;

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1. Antiprotozoal activities of new bicyclo(2.2.2)octan-2-imines and esters of bicyclo(2.2.2)octan-2-ols. [J] . Seebacher W, Schlapper C, Brun R, European journal of pharmaceutical sciences . 2005,第4期

机译：新的双环（2.2.2）辛-2-亚胺和双环（2.2.2）辛-2-醇的酯的抗原生动物活性。
2. Ring effect on helical twisting power of optically active mesogenic esters derived from benzene, bicyclo[2.2.2] octane and p-carborane carboxylic acids [J] . Januszko A, Kaszynski P, Drzewinski W Journal of Materials Chemistry: An Interdisciplinary Journal dealing with Synthesis, Structures, Properties and Applications of Materials, Particulary Those Associated with Advanced Technology . 2006,第5期

机译：环对衍生自苯，双环[2.2.2]辛烷和对-碳烷羧酸的旋光性介晶酯的螺旋扭曲能力的环效应
3. SARs of the antiprotozoal action of 6,7-diaryl-bicyclo[2.2.2]octan-2-ols [J] . Heinrich Berger, Werner Seebacher, Marcel Kaiser, Monatshefte für Chemie / Chemical Monthly . 2009,第5期

机译：SARs对6,7-二芳基-双环[2.2.2] octan-2-ols的抗原生动物作用
4. Preparation of Novel C_2-Symmetric Chiral Bicyclo2.2.2octadiene Ligands and Their Use for Rhodium-Catalyzed Asymmetric 1,4-Addition of Arylboronic Acids [C] . Yusuke Otomaru, Kazuhiro Okamoto, Kazuhito Ueyama, Symposium on Organometallic Chemistry . 2004

机译：新型C_2对称手性双环的制备2.2.2八二烯配体及其用于铑催化的不对称1,4-加入芳基硼酸的用途
5. THE FREE (2.2.2) AND (3.2.1) BICYCLO-2-OCTYL CATIONS. [D] . PLEPYS, RAYMOND ALFONSAS. 1967

机译：自由的（2.2.2）和（3.2.1）的双环-2-辛基阳离子。
6. 14-Diazabicyclo2.2.2octane–transtrans-hexa-24-dienedioic acid (1/1) [O] . Suk-Hee Moon, Ki-Min Park 2012

机译：14-二氮杂双环2.2.2辛烷-反式反-己基24-二烯二酸（1/1）
7. Relationship between experimental pKa values in aqueous solution and a gas phase bond length in bicyclo2.2.2octane and cubane carboxylic acids [O] . Alkorta Ibon, Griffiths Mark Z., Popelier Paul L. A. 2013

机译：水溶液中的实验pKa值与双环2.2.2辛烷和古巴羧酸中的气相键长之间的关系
8. Enolboration 3. An Examination of the Effect of Variable Steric Requirements of R on the Stereoselective Enolboration of Ketones with R2BCl/Et3N. Bis(Bicyclo(2.2.2)Octyl)Chloroborane/Triethylamine - A New Reagent Which Achieves the Selective Generation of [R] . Brown, H. C., Ganesan, K., Dhar, R. K. 1992

机译：Enolboration 3.对R的可变空间要求对R2BCl / Et3N立体选择性烯酮化合物的影响的研究。双（双环（2.2.2）辛基）氯硼烷/三乙胺 - 一种实现选择性生成的新试剂

Bicyclo[2.2.2]octyl esters of dialkylamino acids as antiprotozoals

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