The quinolone-hydroxyquinoline tautomerism in quinolone 3-esters; preserving the 4-oxoquinoline structure to retain antimalarials activity
- Autores: Coelho L, Cristiano ML, 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: http://pubs.acs.org/doi/full/10.1021/acs.joc.5b02169
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 should be investigated.