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Issue 1, 2012
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The development of quinoloneesters as novel antimalarial agents targeting the Plasmodium falciparum bc1 protein complex

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Abstract

Using the Gould-Jacobs methodology a small array of 6- and 7-substituted quinolones have been prepared. Analogues in the 7-series express activity as low as 0.46 nM versus Plasmodium falciparum malaria parasites and docking studies performed in silico at the yeast Qo site demonstrate a key role for residues His182 and Glu 272 in the recognition of high potency inhibitors.

Graphical abstract: The development of quinolone esters as novel antimalarial agents targeting the Plasmodium falciparum bc1 protein complex

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Article information


Submitted
15 Jul 2011
Accepted
15 Aug 2011
First published
01 Sep 2011

Med. Chem. Commun., 2012,3, 39-44
Article type
Concise Article

The development of quinolone esters as novel antimalarial agents targeting the Plasmodium falciparum bc1 protein complex

R. Cowley, S. Leung, N. Fisher, M. Al-Helal, N. G. Berry, A. S. Lawrenson, R. Sharma, A. E. Shone, S. A. Ward, G. A. Biagini and P. M. O′Neill, Med. Chem. Commun., 2012, 3, 39
DOI: 10.1039/C1MD00183C

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