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Title: Azide-alkyne cycloaddition en route to 1H-1,2,3-triazole-tethered 7-chloroquinoline-isatin chimeras : synthesis and antimalarial evaluation
Authors: Raj, Raghu 
Singh, Pardeep 
Singh, Parvesh 
Gut, Jiri 
Rosenthal, Philip J. 
Kumar, Vipan 
Keywords: 7-Chloroquinoline-isatin conjugates;1H-1,2,3-triazole;Antimalarial evaluation;Structure–activity relationship
Issue Date: Apr-2013
Publisher: Elsevier
Source: Raja, 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.
We 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.
DOI: 10.1016/ j.ejmech.2013.01.032
Appears in Collections:Research Publications (Applied Sciences)

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