Twenty two diverse coumarin-triazole derivatives were synthesized by alkylation of 7-hydroxy-4-methyl-coumarin followed by click chemistry at 7-position. These compounds were evaluated for their in vitro antiplasmodial activity against chloroquine sensitive strain of Plasmodium falciparum (3D7). Compound 9 (7-[1-(2, 4-dimethoxy-phenyl)-1H- [1–3] triazol-4-ylmethoxy]-4-methyl-chromen-2-one) was found most active with IC₅₀ value 0.763 ± 0.0124 μg/mL. Further, the structure of compound 20 was characterized by single crystal X-ray diffraction. In view of impressive results, we considered it worthwhile to validate the results of in vitro antiplasmodial activity by assessing whether these compounds are capable of hampering the catalytic activity of DNA gyrase, thus preventing its supercoiling function.

通过将7-羟基-4-甲基-香豆素烷基化，然后在7位进行点击化学反应，合成了22种香豆素-三唑衍生物。评估了这些化合物对恶性疟原虫（3D7）的氯喹敏感菌株的体外抗疟原虫活性。化合物9（7- [1-（2，4-二甲氧基-苯基）-1H- [1-3]三唑-4-基甲氧基] -4-甲基-色烯-2-酮）最具活性，IC ₅₀值为0.763±0.0124μg/ mL。此外，化合物20的结构通过单晶X射线衍射表征。鉴于令人印象深刻的结果，我们认为值得验证体外结果 通过评估这些化合物是否能够抑制DNA促旋酶的催化活性，从而防止其超螺旋功能，从而获得抗血浆活性。