PYRIDINIUM AZOLATE BETAINES AND THEIR DERIVATIVES - A NEW CLASS OF ANTIPROTOZOAL AGENTS

被引:22
作者
ALCALDE, E
DINARES, I
ELGUERO, J
FRIGOLA, J
OSUNA, A
CASTANYS, S
机构
[1] CSIC,INST QUIM MED,E-28006 MADRID,SPAIN
[2] LAB DR ESTEVE SA,E-08026 BARCELONA,SPAIN
[3] UNIV GRANADA,FAC FARM,DEPT PARASITOL,E-18001 GRANADA,SPAIN
关键词
anti-leishmanial activity; N-azolylpyridinium salts; pyridinium azolate mesomeric betaines;
D O I
10.1016/0223-5234(90)90114-I
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
N-azolylpyridinium salts 1 and several betaines of pyridinium azolate 2 have been synthetized in order to study their in vitro antiprotozoal activity. A careful 1H and 13C-NMR study has been carried out in order to characterize the different compounds. A significant growth inhibition of Trypanosoma cruzi and especially Leishmania donovani was observed with the N-benzimidazolyl-pyridinium derivatives. When tested in vivo against Leishmania donovani, compounds 9 and 40 have had a much greater reducing effect in the parasite than that of the reference drug (glucantime). © 1990.
引用
收藏
页码:309 / 319
页数:11
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