Synthesis and in vitro activity of new tetrahydronaphtho[1,2-b]azepine derivatives against Trypanosoma cruzi and Leishmania chagasi parasites.
Series of 2-exo-aryl-1,4-epoxy-2,3,4,5-tetrahydronaphtho[1,2-b]azepines 3a-k and cis-2-aryl-4-hydroxy-2,3,4,5-tetrahydronaphtho[1,2-b]azepines 4a-j were synthesized and evaluated against free and intracellular live forms of Trypanosoma cruzi and Leishmania chagasi parasites using in vitro assays. Cell toxicity was also analyzed on Vero and THP-1 mammalian cell lines. The compounds 3c, 3f, and 4d were the most active against both live forms of T. cruzi parasites with low mammalian cell toxicity. Some compounds were active on free live forms of L. chagasi parasites but none was active on intracellular amastigotes of L. chagasi infecting THP-1 macrophages.
Palma
Alirio
A
Laboratorio de Síntesis Orgánica, Escuela de Química, Universidad Industrial de Santander, Santander, Colombia. apalma@uis.edu.co
Yépes
Andrés Felipe
AF
Leal
Sandra Milena
SM
Coronado
Carlos Andrés
CA
Escobar
Patricia
P