期刊
MEDICINAL CHEMISTRY
卷 3, 期 5, 页码 460-465出版社
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/157340607781745519
关键词
azaheterocyclic derivatives; megazol; Trypanosoma cruzi; Chagas disease; chemotherapy
This study describes the design, synthesis and trypanocidal evaluation of new azaheterocyclic derivatives (4-8). These compounds were designed as megazol (1) analogs based on bioisosterism tools and were synthesized to investigate the possible pharmacophoric contribution of the 1,2,4-triazole nucleus, the position of the heterocyclic nucleus and presence of the nitro group, to the activity against the bloodstream trypomastigote forms of Trypanosoma cruzi. The most potent compound was 6, a nitro derivative obtained by substitution of a thiadiazole by a triazole ring and by moving the nitro group from C-5 position, as in 1, to the C-4 position. Finally, we have used semi-empirical theoretical calculations to discuss the correlation of some stereo electronic properties with biological activity in an attempt to understand the possible mechanism of action of the designed series of compounds.
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