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Home / Archives for Paixão JA

Quinolone-Hydroxyquinoline Tautomerism in Quinolone 3-Esters. Preserving the 4-Oxoquinoline Structure To Retain Antimalarial Activity

  • Autores: Coelho L, Cristiano MLS, Fausto R, Henriques MS, Horta P, Kuş N, Nogueira F, O'Neill PM, Paixão JA
  • Ano de Publicação: 2015
  • Journal: Journal of Organic Chemistry
  • Link: https://pubs.acs.org/doi/10.1021/acs.joc.5b02169%20

Recent publications report in vitro activity of quinolone 3-esters against the bc1 protein complex of Plasmodium falciparum and the parasite. Docking studies performed in silico at the yeast Qo site established a key role for the 4-oxo and N-H groups in drug-target interactions. Thus, the possibility of 4-oxoquinoline/4-hydroxyquinoline tautomerism may impact in pharmacologic profiles and […]
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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

  • Autores: Brás EM, Cristiano MLS, Fausto R, Henriques MSC, Horta P, Murtinheira F, Nogueira F, O'Neill PM, Paixão JA
  • Ano de Publicação: 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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About GHTM

GHTM is a R&D Center that brings together researchers from IHMT with a track record in Tropical Medicine and International/Global Health. It aims at strengthening Portugal's role as a leading partner in the development and implementation of a global health research agenda. Our evidence-based interventions contribute to the promotion of equity in health and to improve the health of populations.

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