1. Synthesis, antimycobacterial and cytotoxic activity of α,β-unsaturated amides and 2,4-disubstituted oxazoline derivatives.
- Author
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Avalos-Alanís, Francisco G., Hernández-Fernández, Eugenio, Carranza-Rosales, Pilar, López-Cortina, Susana, Hernández-Fernández, Jorge, Ordóñez, Mario, Guzmán-Delgado, Nancy E., Morales-Vargas, Alejandro, Velázquez-Moreno, Víctor M., and Santiago-Mauricio, María G.
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CHEMICAL synthesis , *OXAZOLINE derivatives , *MYCOBACTERIUM tuberculosis , *TUBERCULOSIS treatment , *HEPATOTOXICOLOGY - Abstract
The synthesis of six α,β,-unsaturated amides and six 2,4-disubstituted oxazolines derivatives and their evaluation against two Mycobacterium tuberculosis strains (sensitive H37Rv and a resistant clinical isolate) is reported. 2,4-Disubstituted oxazolines ( S )- 3b,d,e were the most active in the sensitive strain with a MIC of 14.2, 13.6 and 10.8 μM, respectively, and the compounds ( S )- 3d , f were the most active against resistant strain with a MIC of 6.8 and 7.4 μM. The ex-vivo evaluation of hepatotoxicity on precision-cut rat liver slices was also tested for the α,β-unsaturated amides ( S )- 2b and ( S )- 2d , f and for the oxazolines ( S )- 3b and ( S )- 3d,f at different concentrations (5, 15 and 30 μg/mL). The results indicate that these compounds possess promising antimycobacterial activity and at the same time are not hepatotoxic. These findings open the possibility for development of new drugs against tuberculosis. [ABSTRACT FROM AUTHOR]
- Published
- 2017
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