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

Robin Cowley; Suet Leung; Nicholas Fisher; Mohammed Al-Helal; Neil G. Berry; Alexandre S. Lawrenson; Raman Sharma; Alison E. Shone; Steve Ward; Giancarlo Biagini; Paul M. O'Neill

doi:10.1039/c1md00183c

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

Robin Cowley, Suet Leung, Nicholas Fisher, Mohammed Al-Helal, Neil G. Berry, Alexandre S. Lawrenson, Raman Sharma, Alison E. Shone, Steve Ward, Giancarlo Biagini, Paul M. O'Neill

Tropical Disease Biology

Research output: Chapter in Book/Report/Conference proceeding › Conference contribution › peer-review

35 Citations (Scopus)

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.

Original language	English
Title of host publication	RSC Medicinal Chemistry
Publisher	Royal Society of Chemistry
Pages	39-44
Number of pages	6
Volume	3
Edition	1
DOIs	https://doi.org/10.1039/c1md00183c
Publication status	Published - 1 Mar 2012

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10.1039/c1md00183c

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Cowley, R., Leung, S., Fisher, N., Al-Helal, M., Berry, N. G., Lawrenson, A. S., Sharma, R., Shone, A. E., Ward, S., Biagini, G., & O'Neill, P. M. (2012). The development of quinolone esters as novel antimalarial agents targeting the Plasmodium falciparum bc1 protein complex. In RSC Medicinal Chemistry (1 ed., Vol. 3, pp. 39-44). Royal Society of Chemistry. https://doi.org/10.1039/c1md00183c

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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.",

author = "Robin Cowley and Suet Leung and Nicholas Fisher and Mohammed Al-Helal and Berry, {Neil G.} and Lawrenson, {Alexandre S.} and Raman Sharma and Shone, {Alison E.} and Steve Ward and Giancarlo Biagini and O'Neill, {Paul M.}",

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Cowley, R, Leung, S, Fisher, N, Al-Helal, M, Berry, NG, Lawrenson, AS, Sharma, R, Shone, AE, Ward, S , Biagini, G & O'Neill, PM 2012, The development of quinolone esters as novel antimalarial agents targeting the Plasmodium falciparum bc1 protein complex. in RSC Medicinal Chemistry. 1 edn, vol. 3, Royal Society of Chemistry, pp. 39-44. https://doi.org/10.1039/c1md00183c

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T1 - The development of quinolone esters as novel antimalarial agents targeting the Plasmodium falciparum bc1 protein complex

AU - Cowley, Robin

AU - Leung, Suet

AU - Fisher, Nicholas

AU - Al-Helal, Mohammed

AU - Berry, Neil G.

AU - Lawrenson, Alexandre S.

AU - Sharma, Raman

AU - Shone, Alison E.

AU - Ward, Steve

AU - Biagini, Giancarlo

AU - O'Neill, Paul M.

PY - 2012/3/1

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N2 - 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.

AB - 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.

U2 - 10.1039/c1md00183c

DO - 10.1039/c1md00183c

M3 - Conference contribution

VL - 3

SP - 39

EP - 44

BT - RSC Medicinal Chemistry

PB - Royal Society of Chemistry

ER -

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

Abstract

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