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

Cowley, Robin, Leung, Suet, Fisher, Nicholas, Al-Helal, Mohammed, Berry, Neil G., Lawrenson, Alexandre S., Sharma, Raman, Shone, Alison, Ward, Stephen ORCID: https://orcid.org/0000-0003-2331-3192, Biagini, Giancarlo ORCID: https://orcid.org/0000-0001-6356-6595 and O′Neill, Paul M. (2012) 'The development of quinolone esters as novel antimalarial agents targeting the Plasmodium falciparum bc1 protein complex'. MedChemComm, Vol 3, Issue 1, pp. 39-44.

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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.

Item Type: Article
Subjects: QV Pharmacology > Anti-Inflammatory Agents. Anti-Infective Agents. Antineoplastic Agents > QV 250 Anti-infective agents (General)
QV Pharmacology > Anti-Inflammatory Agents. Anti-Infective Agents. Antineoplastic Agents > QV 256 Antimalarials
QX Parasitology > Protozoa > QX 135 Plasmodia
WC Communicable Diseases > Tropical and Parasitic Diseases > WC 750 Malaria
WC Communicable Diseases > Tropical and Parasitic Diseases > WC 765 Prevention and control
Faculty: Department: Groups (2002 - 2012) > Molecular & Biochemical Parasitology Group
Digital Object Identifer (DOI): https://doi.org/10.1039/c1md00183c
Depositing User: Lynn Roberts-Maloney
Date Deposited: 19 Dec 2014 09:38
Last Modified: 06 Feb 2018 13:08
URI: https://archive.lstmed.ac.uk/id/eprint/4689

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