In vitro activities of DU-1102, a new trioxaquine derivative, against Plasmodium falciparum isolates.
作者信息
Basco L K, Dechy-Cabaret O, Ndounga M, Meche F S, Robert A, Meunier B
机构信息
Institut de Recherche pour le Développement-Laboratoire de Recherche sur le Paludisme, Organisation de Coordination pour la lutte contre les Endémies en Afrique Centrale (OCEAC), Yaoundé, Cameroon.
出版信息
Antimicrob Agents Chemother. 2001 Jun;45(6):1886-8. doi: 10.1128/AAC.45.6.1886-1888.2001.
Abstract
The antimalarial trioxaquine derivative DU-1102, synthesized by covalent linkage between aminoquinoline and trioxane moieties, was highly active against Cameroonian isolates (mean 50% inhibitory concentration of 43 nmol/liter) of Plasmodium falciparum. There was no correlation between the responses to DU-1102 and chloroquine and only a low correlation between the responses to DU-1102 and pyrimethamine, suggesting an independent mode of action of the trioxaquine against the parasites.
摘要
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本文引用的文献
1
Strategies for the prevention of antimalarial drug resistance: rationale for combination chemotherapy for malaria.
Parasitol Today. 1996 Oct;12(10):399-401. doi: 10.1016/0169-4758(96)10055-7.
2
Preparation and antimalarial activities of "trioxaquines", new modular molecules with a trioxane skeleton linked to a 4-aminoquinoline.
Chembiochem. 2000 Nov 17;1(4):281-3. doi: 10.1002/1439-7633(20001117)1:4<281::AID-CBIC281>3.0.CO;2-W.
3
Molecular epidemiology of malaria in Yaounde, Cameroon IV. Evolution of pyrimethamine resistance between 1994 and 1998.
Am J Trop Med Hyg. 1999 Nov;61(5):802-6. doi: 10.4269/ajtmh.1999.61.802.
4
Current progress in the chemistry, medicinal chemistry and drug design of artemisinin based antimalarials.
Curr Pharm Des. 1999 Feb;5(2):101-38.
5
In vitro activity of lumefantrine (benflumetol) against clinical isolates of Plasmodium falciparum in Yaoundé, Cameroon.
Antimicrob Agents Chemother. 1998 Sep;42(9):2347-51. doi: 10.1128/AAC.42.9.2347.
6
Design, synthesis, derivatization, and structure-activity relationships of simplified, tricyclic, 1,2,4-trioxane alcohol analogues of the antimalarial artemisinin.
J Med Chem. 1998 Mar 12;41(6):952-64. doi: 10.1021/jm970711g.
7
Antimalarial activity of artemisinin (qinghaosu) and related trioxanes: mechanism(s) of action.
Adv Pharmacol. 1997;37:253-97. doi: 10.1016/s1054-3589(08)60952-7.
8
Artemisinin and the antimalarial endoperoxides: from herbal remedy to targeted chemotherapy.
Microbiol Rev. 1996 Jun;60(2):301-15. doi: 10.1128/mr.60.2.301-315.1996.
9
Randomised trial of pyronaridine versus chloroquine for acute uncomplicated falciparum malaria in Africa.
Lancet. 1996 Jan 6;347(8993):24-8. doi: 10.1016/s0140-6736(96)91558-5.
10
Structure-activity relationships of the antimalarial agent artemisinin. 1. Synthesis and comparative molecular field analysis of C-9 analogs of artemisinin and 10-deoxoartemisinin.
J Med Chem. 1993 Dec 24;36(26):4264-75. doi: 10.1021/jm00078a017.
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