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.

中文翻译：

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磺酰胺基香豆素-[1,2,3]-三唑的合成及抗疟活性

疟原虫的耐药性是阻碍消除疟疾目标的主要绊脚石之一。抗药性的主要策略之一是开发新的有效抗疟药。在本研究中，通过叠氮磺酰胺与4-羟基-或7-羟基甲基香豆素炔之间的Huisgen反应合成了一系列基于磺酰胺的香豆素-[1,2,3]-三唑共轭物。已对所有化合物进行了光谱表征，并筛选了它们对恶性疟原虫3D7菌株的体外抗疟活性。在这25种合成化合物中，四种化合物表现出显着的活性（IC ₅₀ <10 µM），而活性最高的化合物具有IC₅₀ of 3.64 µM。