A novel artemisinin-quinine hybrid with potent antimalarial activity

被引:140
作者
Walsh, John J. [1 ]
Coughlana, David
Heneghan, Nicola
Gaynor, Caroline
Bell, Angus
机构
[1] Univ Dublin Trinity Coll, Sch Pharm & Pharmaceut Sci, Dublin 2, Ireland
[2] Univ Dublin Trinity Coll, Moyne Inst Prevent Med, Dept Microbiol, Dublin 2, Ireland
关键词
D O I
10.1016/j.bmcl.2007.04.054
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Artemisinin was reduced to dihydroartemisinin and coupled to a carboxylic acid derivative of quinine via an ester linkage. This novel hybrid molecule had potent activity against the 3D7 and (drug-resistant) FcB1 strains of Plasmodium falciparum? in culture. The activity was superior to that of artemisinin alone, quinine alone, or a 1:1 mixture of artemisinin and quinine. (c) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3599 / 3602
页数:4
相关论文
共 16 条
[1]  
AVERY MA, 1999, ADV MED CH, V4, P125
[2]   In vitro activities of DU-1102, a new trioxaquine derivative, against Plasmodium falciparum isolates [J].
Basco, LK ;
Dechy-Cabaret, O ;
Ndounga, M ;
Meche, FS ;
Robert, A ;
Meunier, B .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 2001, 45 (06) :1886-1888
[3]   Antimalarial drug synergism and antagonism: Mechanistic and clinical significance [J].
Bell, A .
FEMS MICROBIOLOGY LETTERS, 2005, 253 (02) :171-184
[4]  
Bray PG, 2005, CURR TOP MICROBIOL, V295, P3
[5]   Antimalarial drug therapy: The role of parasite biology and drug resistance [J].
Daily, Johanna P. .
JOURNAL OF CLINICAL PHARMACOLOGY, 2006, 46 (12) :1487-1497
[6]   Combinations of artemisinin and quinine for uncomplicated falciparum malaria: Efficacy and pharmacodynamics [J].
de Vries, PJ ;
Bich, NN ;
van Thien, H ;
Hung, LN ;
Anh, TK ;
Kager, PA ;
Heisterkamp, SH .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 2000, 44 (05) :1302-1308
[7]  
Dechy-Cabaret O, 2000, CHEMBIOCHEM, V1, P281, DOI 10.1002/1439-7633(20001117)1:4<281::AID-CBIC281>3.0.CO
[8]  
2-W
[9]   Artemisinins target the SERCA of Plasmodium falciparum [J].
Eckstein-Ludwig, U ;
Webb, RJ ;
van Goethem, IDA ;
East, JM ;
Lee, AG ;
Kimura, M ;
O'Neill, PM ;
Bray, PG ;
Ward, SA ;
Krishna, S .
NATURE, 2003, 424 (6951) :957-961
[10]  
Faiz MA, 2005, LANCET, V366, P717