The effect of fluorine substitution on the antimalarial activity of tebuquine

被引：9

作者：

ONeill, PM ^{[1
]}

Hawley, SR ^{[1
]}

Storr, RC ^{[1
]}

Ward, SA ^{[1
]}

Park, BK ^{[1
]}

机构：

[1] UNIV LIVERPOOL, DEPT CHEM, LIVERPOOL L69 3BX, MERSEYSIDE, ENGLAND

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 04期

基金：

英国惠康基金;

关键词：

D O I：

10.1016/0960-894X(96)00040-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel synthetic route has been developed for the synthesis of fluorotebuquine which was active against the chloroquine resistant K1 strain of Plasmodium Falciparum, but less potent than both chloroquine and tebuquine against the 3D7 strain.

引用

页码：391 / 392

页数：2

共 7 条

[1]

BALTZ G, 1927, BER DTSCH CHEM GES, V60, P1186

[2] 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

[3] THE MECHANISM OF BIOACTIVATION AND ANTIGEN FORMATION OF AMODIAQUINE IN THE RAT [J].

HARRISON, AC ;

KITTERINGHAM, NR ;

CLARKE, JB ;

PARK, BK .

BIOCHEMICAL PHARMACOLOGY, 1992, 43 (07) :1421-1430

[4] PLASMODIUM-FALCIPARUM IN CULTURE - USE OF OUTDATED ERYTHROCYTES AND DESCRIPTION OF CANDLE JAR METHOD [J].

JENSEN, JB ;

TRAGER, W .

JOURNAL OF PARASITOLOGY, 1977, 63 (05) :883-886

[5] THE PALLADIUM-CATALYZED CROSS-COUPLING REACTION OF PHENYLBORONIC ACID WITH HALOARENES IN THE PRESENCE OF BASES [J].

MIYAURA, N ;

YANAGI, T ;

SUZUKI, A .

SYNTHETIC COMMUNICATIONS, 1981, 11 (07) :513-519

[6] THE EFFECT OF FLUORINE SUBSTITUTION ON THE METABOLISM AND ANTIMALARIAL ACTIVITY OF AMODIAQUINE [J].

ONEILL, PM ;

HARRISON, AC ;

STORR, RC ;

HAWLEY, SR ;

WARD, SA ;

PARK, BK .

JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (09) :1362-1370

[7] ANTIMALARIAL-DRUGS .60. SYNTHESIS, ANTIMALARIAL ACTIVITY, AND QUANTITATIVE STRUCTURE-ACTIVITY-RELATIONSHIPS OF TEBUQUINE AND A SERIES OF RELATED 5-[(7-CHLORO-4-QUINOLINYL)AMINO]-3-[(ALKYLAMINO)METHYL][1,1'-BIPHENYL]-2-OLS AND N-OMEGA-OXIDES1,2 [J].

WERBEL, LM ;

COOK, PD ;

ELSLAGER, EF ;

HUNG, JH ;

JOHNSON, JL ;

KESTEN, SJ ;

MCNAMARA, DJ ;

ORTWINE, DF ;

WORTH, DF .

JOURNAL OF MEDICINAL CHEMISTRY, 1986, 29 (06) :924-939

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