Formula: C5H5BrN2In 2019 ,《Identification of novel quinazoline derivatives as potent antiplasmodial agents》 appeared in European Journal of Medicinal Chemistry. The author of the article were Bouchut, Anne; Rotili, Dante; Pierrot, Christine; Valente, Sergio; Lafitte, Sophia; Schultz, Johan; Hoglund, Urban; Mazzone, Roberta; Lucidi, Alessia; Fabrizi, Giancarlo; Pechalrieu, Dany; Arimondo, Paola B.; Skinner-Adams, Tina S.; Chua, Ming Jang; Andrews, Kathy T.; Mai, Antonello; Khalife, Jamal. The article conveys some information:
Despite the recent reductions in the global burden of malaria, this disease remains a devastating cause of death in tropical and subtropical regions. As there is no broadly effective vaccine for malaria, prevention and treatment still rely on chemotherapy. Unfortunately, emerging resistance to the gold standard artemisinin combination therapies means that new drugs with novel modes of action are urgently needed. In this context, Plasmodium histone modifying enzymes have emerged as potential drug targets, prompting us to develop and optimize compounds directed against such epigenetic targets. A panel of 51 compounds designed to target different epigenetic enzymes were screened for activity against Plasmodium falciparum parasites. Based on in vitro activity against drug susceptible and drug-resistant P. falciparum lines, selectivity index criterion and favorable pharmacokinetic properties, four compounds, one HDAC inhibitor (1) and three DNMT inhibitors (37, 43 and 45), were selected for preclin. studies in a mouse model of malaria. In vivo data showed that 37, 43 and 45 exhibited oral efficacy in the mouse model of Plasmodium berghei infection. These compounds represent promising starting points for the development of novel antimalarial drugs. In the part of experimental materials, we found many familiar compounds, such as 6-Bromopyridin-3-amine(cas: 13534-97-9Formula: C5H5BrN2)
6-Bromopyridin-3-amine(cas: 13534-97-9) belongs to anime. Examples of direct uses of amines and their salts are as corrosion inhibitors in boilers and in lubricating oils (morpholine), as antioxidants for rubber and roofing asphalt (diarylamines), as stabilizers for cellulose nitrate explosives (diphenylamine), as protectants against damage from gamma radiation (diarylamines), as developers in photography (aromatic diamines), as flotation agents in mining, as anticling and waterproofing agents for textiles, as fabric softeners, in paper coating, and for solubilizing herbicides.Formula: C5H5BrN2