Azide-alkyne cycloaddition en route to 1H-1,2,3-triazole-tethered 7-chloroquinoline-isatin chimeras: Synthesis and antimalarial evaluation

Abstract We describe the synthesis and antimalarial activities of 1 H -1,2,3-triazole tethered 7-chloroquinoline-isatin hybrids. Activity against cultured parasites was dependent on the C-5 substituent of the isatin ring as well as the alkyl chain length between the isatin and 7-chloroquinoline moieties. Compound 8h , with an optimum alkyl chain length ( n  = 3) and a chloro substituent at the C-5 position of the isatin ring, displayed the best activity among the test compounds, with IC 50 value of 1.21 μM against cultured W2-strain Plasmodium falciparum .