期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 39, 期 7, 页码 639-645出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2004.02.015
关键词
Trypanosoma cruzi; Chagas' disease; naphthoquinones; beta-lapachone; naphthoimidazoles; chemotherapy
We synthesized new naphthoimidazoles from beta-lapachone with an aromatic moiety linked to the imidazole ring, using phenylic and heterocyclic aldehydes. The most active compound against Typanosoma cruzi had a p-methyl group linked to the phenyl ring, presenting an EC50 value of 15.5 +/- 2.9 muM. No reliable correlation could be established with the biological activity and the structure of in the phenylic series. For the heterocyclic series, activity was associated with a three bond-distance from nitrogen to the imidazole ring, in accordance with our previous work. (C) 2004 Elsevier SAS. All rights reserved.
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