On the ordeal of quinolone preparation via cyclisation of aryl-enamines; Synthesis and structure of ethyl 6-methyl-7-iodo-4-(3-iodo-4-methylphenoxy)-quinoline-3-carboxylate

• Authors: Brás EM, Cristiano MLS, Fausto R, Henriques MSC, Horta P, Murtinheira F, Nogueira F, O'Neill PM, Paixão JA
• Publication Year: 2017
• Journal: Pure and Applied Chemistry
• Link: https://www.degruyter.com/view/j/pac.2017.89.issue-6/pac-2016-1119/pac-2016-1119.xml

Recent studies directed to the design of compounds targeting the bc1 protein complex of Plasmodium falciparum, the parasite responsible for most lethal cases of malaria, identified quinolones (4-oxo-quinolines) with low nanomolar inhibitory activity against both the enzyme and infected erythrocytes. The 4-oxo-quinoline 3-ester chemotype emerged as a possible source of potent bc1 inhibitors, prompting us to expand the library of available […]
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