9-ANILINOACRIDINES AS POTENTIAL ANTILEISHMANIAL AGENTS

被引:29
作者
MAUEL, J
DENNY, W
GAMAGE, S
RANSIJN, A
WOJCIK, S
FIGGITT, D
RALPH, R
机构
[1] UNIV AUCKLAND,DEPT CELLULAR & MOLEC BIOL,PRIVATE BAG 92019,AUCKLAND,NEW ZEALAND
[2] UNIV AUCKLAND,CANC RES LAB,AUCKLAND,NEW ZEALAND
[3] UNIV LAUSANNE,INST BIOCHEM,CH-1066 EPALINGES,SWITZERLAND
关键词
D O I
10.1128/AAC.37.5.991
中图分类号
Q93 [微生物学];
学科分类号
071005 ; 100705 ;
摘要
A number of 1'-substituted 9-anilinoacridines were evaluated for their activities against promastigote and amastigote forms of Leishmania major and for their toxicities to human Jurkat leukemia cells. Several compounds possessing 1'-NH-alkyl substituents produced more than 80% growth inhibition of macrophage-infected L. major amastigotes at or below a concentration of 1 muM. 1'-Hexylamino-9-anilinoacridine (compound 14) was the least toxic compound to human Jurkat cells, while it retained strong antileishmanial activity. There was a general trend for the more lipophilic compounds to show the greatest antileishmanial activity, whereas 3,6-di-NH2 substitution of the acridine nucleus reduced or eliminated activity. Some structure-activity relationships of the various compounds are discussed.
引用
收藏
页码:991 / 996
页数:6
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