In vitro antiplasmodial efficacy of synthetic coumarin-triazole analogs

作者：Yadav Neesha; Agarwal Drishti; Kumar Satyanand; Dixit A K; Gupta Rinkoo D; Awasthi Satish K^*

来源：European Journal of Medicinal Chemistry, 2018, 145: 735-745.

DOI：10.1016/j.ejmech.2018.01.017

• Coumarin
• Plasmodium falciparum
• Antiplasmodial
• DNA gyrase

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 mu g/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.

• 出版日期2018-2-10