93919-57-4Relevant academic research and scientific papers
Unsymmetrical bisquinolines with high potency against P. falciparum Malaria
Burgess, Steven J.,Gunsaru, Bornface,Kelly, Jane X.,Li, Yuexin,Liebman, Katherine M.,Liebman, Michael C.,Morrill, Westin,Peyton, David H.
supporting information, (2020/05/18)
Quinoline-based scaffolds have been the mainstay of antimalarial drugs, including many artemisinin combination therapies (ACTs), over the history ofmoderndrugdevelopment. Althoughmuch progress has beenmade in the search for novel antimalarial scaffolds, itmay be that quinolineswill remain useful, especially if very potent compounds fromthis class are discovered. We report here the results of a structure-activity relationship(SAR) study assessingpotentialunsymmetrical bisquinoline antiplasmodial drug candidates using in vitro activity against intact parasites in cell culture. Many unsymmetrical bisquinolineswere found to be highly potent against both chloroquine-sensitive and chloroquine-resistant Plasmodium falciparum parasites. Further work to develop such compounds could focus on minimizing toxicities in order to find suitable candidates for clinical evaluation.
Coordinating Activation Strategy-Induced Selective C?H Trifluoromethylation of Anilines
Xu, Jun,Cheng, Ke,Shen, Chao,Bai, Renren,Xie, Yuanyuan,Zhang, Pengfei
, p. 965 - 970 (2018/02/12)
A simple protocol for the synthesis of 2-(trifluoromethyl)aniline derivatives through a coordinating activation strategy was developed. The reaction showed good reactivity and gave the target products in moderate to good yields. Pleasingly, the directing group could be recovered in excellent yield. Furthermore, this strategy allowed efficient access to the synthesis of floctafenine. A single-electron-transfer mechanism was proposed to be responsible for this trifluoromethylation reaction.
Synthesis of novel halogenated 4(1H)-quinolones by thermolysis of arylaminomethylene-1,3-dioxane-4,6-diones
Rotzoll, Sven,Reinke, Helmut,Fischer, Christine,Langer, Peter
experimental part, p. 69 - 78 (2009/06/17)
A variety of novel 4(1H)-quinolone derivatives were prepared by thermolysis of aminomethylene Meldrum's acid derivatives. Georg Thieme Verlag Stuttgart.
