136672-34-9Relevant articles and documents
In vitro antiplasmodial efficacy of synthetic coumarin-triazole analogs
Yadav, Neesha,Agarwal, Drishti,Kumar, Satyanand,Dixit,Gupta, Rinkoo D.,Awasthi, Satish K.
, p. 735 - 745 (2018)
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.
Intramolecular Carbonylative C–H Functionalization of 1,2,3- Triazoles for the Synthesis of Triazolo[1,5-a]indolones
Veryser, Cedrick,Steurs, Gert,Van Meervelt, Luc,De Borggraeve, Wim M.
supporting information, p. 1271 - 1276 (2017/04/18)
This study presents a synthesis of 4H-[1,2,3]triazolo[1,5-a]indol-4-ones. The key step in the synthesis of this new heterocyclic scaffold is an intramolecular cyclization via an unprecedented carbonylative C–H functionalization of 1-(2-bromoaryl)-1,2,3-tr
In situ "click" assembly of small molecule matrix metalloprotease inhibitors containing zinc-chelating groups
Hu, Mingyu,Li, Junqi,Yao, Shao Q.
supporting information; experimental part, p. 5529 - 5531 (2009/06/17)
(Chemical Equation Presented) A panel of small molecule-based MMP inhibitors containing rhodanine warheads was assembled using "one-pot" click chemistry. Upon biological screening, moderate inhibitors were identified which specifically targets MMP-7 and MMP-13 over other MMPs.
