INVITRO ACTIVITY OF THE ENANTIOMERS OF MEFLOQUINE, HALOFANTRINE AND ENPIROLINE AGAINST PLASMODIUM-FALCIPARUM

被引:58
作者
BASCO, LK
GILLOTIN, C
GIMENEZ, F
FARINOTTI, R
LEBRAS, J
机构
[1] HOP LA PITIE SALPETRIERE,DEPT PHARM & PHARMACOKINET,F-75013 PARIS,FRANCE
[2] HOP BICHAT CLAUDE BERNARD,DEPT CLIN PHARM,F-75018 PARIS,FRANCE
关键词
PLASMODIUM-FALCIPARUM; MALARIA; MEFLOQUINE; HALOFANTRINE; ENPIROLINE; ENANTIOMERS;
D O I
10.1111/j.1365-2125.1992.tb04081.x
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The in vitro activity of the enantiomers of mefloquine, halofantrine and enpiroline was compared against chloroquine-resistant and -susceptible strains of Plasmodium falciparum using a semi-micro drug susceptibility test. For each strain, the corresponding enantiomers exhibited similar activities. The enantiomers of halofantrine were the most active against both susceptible and resistant strains, followed by the enantiomers of mefloquine and enpiroline.
引用
收藏
页码:517 / 520
页数:4
相关论文
共 13 条
[1]   RESOLUTION OF ANTI-MALARIAL AGENTS VIA COMPLEX-FORMATION WITH ALPHA-(2,4,5,7-TETRANITRO-9-FLUORENYLIDENEAMINOOXY)PROPIONIC ACID [J].
CARROLL, FI ;
BERRANG, B ;
LINN, CP .
JOURNAL OF MEDICINAL CHEMISTRY, 1978, 21 (04) :326-330
[2]   OPTICAL ISOMERS OF ARYL-2-PIPERIDYLMETHANOL ANTIMALARIAL AGENTS - PREPARATION, OPTICAL PURITY, AND ABSOLUTE STEREOCHEMISTRY [J].
CARROLL, FI ;
BLACKWELL, JT .
JOURNAL OF MEDICINAL CHEMISTRY, 1974, 17 (02) :210-219
[3]   EVALUATION OF THE 4-PYRIDINEMETHANOL WR-180,409 (ENPIROLINE) IN THE TREATMENT OF INDUCED PLASMODIUM-FALCIPARUM INFECTIONS IN HEALTHY, NON-IMMUNE SUBJECTS [J].
COSGRIFF, TM ;
BOUDREAU, EF ;
PAMPLIN, CL ;
BERMAN, JD ;
SHMUKLARSKY, MJ ;
CANFIELD, CJ .
AMERICAN JOURNAL OF TROPICAL MEDICINE AND HYGIENE, 1984, 33 (05) :767-771
[4]   QUANTITATIVE ASSESSMENT OF ANTI-MALARIAL ACTIVITY INVITRO BY A SEMIAUTOMATED MICRODILUTION TECHNIQUE [J].
DESJARDINS, RE ;
CANFIELD, CJ ;
HAYNES, JD ;
CHULAY, JD .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1979, 16 (06) :710-718
[5]  
FU S, 1986, BRIT J CLIN PHARMACO, V22, P93
[6]   DETERMINATION OF THE ENANTIOMERS OF MEFLOQUINE IN PLASMA AND WHOLE-BLOOD USING A COUPLED ACHIRAL CHIRAL HIGH-PERFORMANCE LIQUID-CHROMATOGRAPHIC SYSTEM [J].
GIMENEZ, F ;
FARINOTTI, R ;
THUILLIER, A ;
HAZEBROUCQ, G ;
WAINER, IW .
JOURNAL OF CHROMATOGRAPHY-BIOMEDICAL APPLICATIONS, 1990, 529 (02) :339-346
[7]  
GIMENEZ F, 1992, IN PRESS J PHARM BIO
[8]   CRYSTAL AND MOLECULAR-STRUCTURE OF THE ANTIMALARIAL AGENT ENPIROLINE [J].
KARLE, JM ;
KARLE, IL .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1989, 33 (07) :1081-1089
[9]  
LEBRAS J, 1983, AM J TROP MED HYG, V32, P447
[10]   ANTI-MALARIAL ACTIVITIES OF VARIOUS 4-QUINOLINEMETHANOLS WITH SPECIAL ATTENTION TO WR-142,490 (MEFLOQUINE) [J].
SCHMIDT, LH ;
CROSBY, R ;
RASCO, J ;
VAUGHAN, D .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1978, 13 (06) :1011-1030