Abstract
In this study, hybrids 7–12 and 19–24 were synthesized via Williamson reaction of O-Quinaldine alkyl bromide plus eugenol and O-triclosan alkyl bromide plus 8-hydroxyquinaldine, respectively. Structures of the products were elucidated by spectroscopic analysis. The compounds synthesized were evaluated for antileishmanial activity against L. panamensis amastigotes and cytotoxic activity against U-937 cells. The compounds 19, 20, and 21 that are 8-hydroxyquinaldine linked to triclosan by 3, 4, and 5-carbon space, respectively, were more active against axenic amastigotes (EC 50 = 23.6, 9.7, and 4.1 μg/ml, respectively). Compounds 19 and 21 were also active against intracellular amastigotes with EC 50 vales of 6.4 and 2.4 μg/ml, respectively, making these compounds promising for the development of new antileishmanial drugs. Quinoline–triclosan and quinoline–eugenol hybrids were obtained using Williamson etherification reactions. Leishmanicidal activity and cytotoxicity of these compounds are reported.
Published Version
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