
Bioorganic and Medicinal Chemistry Letters p. 821 - 825 (2017)
Update date:2022-09-26
Topics:
Avalos-Alanís, Francisco G.
Hernández-Fernández, Eugenio
Carranza-Rosales, Pilar
López-Cortina, Susana
Hernández-Fernández, Jorge
Ordó?ez, Mario
Guzmán-Delgado, Nancy E.
Morales-Vargas, Alejandro
Velázquez-Moreno, Víctor M.
Santiago-Mauricio, María G.
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.
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