title: Synthesis and in vitro activity of new tetrahydronaphtho[1,2-b]azepine derivatives against Trypanosoma cruzi and Leishmania chagasi parasites.
abstract: 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.
authors.affiliation: Laboratorio de Síntesis Orgánica, Escuela de Química, Universidad Industrial de Santander, Santander, Colombia. apalma@uis.edu.co
authors.forename: Alirio
authors.initials: A
authors.lastname: Palma
authors.forename: Andrés Felipe
authors.initials: AF
authors.lastname: Yépes
authors.forename: Sandra Milena
authors.initials: SM
authors.lastname: Leal
authors.forename: Carlos Andrés
authors.initials: CA
authors.lastname: Coronado
authors.forename: Patricia
authors.initials: P
authors.lastname: Escobar