Raj, RaghuSingh, PardeepSingh, ParveshGut, JiriRosenthal, Philip J.Kumar, Vipan2013-08-292013-08-292013-04Raja, R., Singh, P., Singh, P., Gutc, J., Rosenthalc, P.J. and Kumar, V. 2013. Azide-alkyne cycloaddition en route to 1H-1,2,3-triazole-tethered 7-chloroquinoline-isatin chimeras: Synthesis and antimalarial evaluation. European Journal of Medicinal Chemistry, 62: 590–596.http://hdl.handle.net/10321/893We describe the synthesis and antimalarial activities of 1H-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 IC50 value of 1.21 μM against cultured W2-strain Plasmodium falciparum.7 pen7-Chloroquinoline-isatin conjugates1H-1,2,3-triazoleAntimalarial evaluationStructure–activity relationshipMalariaArticle10.1016/ j.ejmech.2013.01.032