Potent Anti-Malaria Salts, Co-Crystals and Derivatives of Aminoquinolines with Hydroxyaromatic Acids

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作者
Baruah, J. B. [1 ]
Khakhlary, P. [1 ]
Holland, S. [2 ]
van Zyl, R. L. [2 ]
机构
[1] Indian Inst Technol, Dept Chem, Gauhati 781039, Assam, India
[2] Univ Witwatersrand, Div Pharmacol, Dept Pharm & Pharmacol, Fac Hlth Sci,WITS Res,Inst Malaria WRIM, Johannesburg, South Africa
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中图分类号
Q81 [生物工程学(生物技术)]; Q93 [微生物学];
学科分类号
071005 ; 0836 ; 090102 ; 100705 ;
摘要
Antimalarial activities of salts of aminoquinolines with hydroxyaromatic acids were found to be higher than the parent components. The IC50 values of the salts were in the range of 5.9-20.3 mu M against the chloroquine-resistant strain. Antimalarial actions on the parasites were found to be independent of iron chelation, inhibition of haemozoin formation, as well as independent of the anti-oxidant activity of the salts. A covalently linked amide containing compound N-(quinolin-8-yl)-2-(quinolin-8-yloxy)acetamide was identified to have potency similar to the other salts studied in the article.
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页码:31 / 35
页数:5
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