Synthesis and antimalarial activity of sulfonamide-attached coumarin-[1,2,3]-triazoles


Nath, Mahendra ; Wadi, Ishan ; Nath, Mahendra ; Rajendran, Vinoth ; Ghosh, C


Drug resistance in malaria parasites is one of the major stumbling blocks hindering the goal of malaria elimination. One of the major strategies to counter drug resistance is the development of new potent antimalarial drugs. In the present study, a series of novel sulfonamide based coumarin-[1,2,3]-triazole conjugates have been synthesized via Huisgen reaction between azidosulfonamides and 4-hydroxy- or 7-hydroxymethylcoumarinoalkynes. All the compounds have been characterized spectroscopically and screened for their in vitro antimalarial activity against P. falciparum 3D7 strain. Out of the twenty five synthesized compounds, four compounds displayed significant activity (IC50 <10 µM) with the most active compound having an IC50 of 3.64 µM.



Antimalarial activity, 4-hydroxycoumarin, 7-hydroxycoumarin, Huisgen [3+2] cycloaddition, sulfonamides, [1,2,3]-triazoles

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