The development of quinoloneesters as novel antimalarial agents targeting the Plasmodium falciparum bc<sub>1</sub>protein complex

Name: Work Video:
Duration: 3 min 30 s
Description: 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.
Robin Neil Cowley; Suet C. Leung; Nicholas Fisher; Mohammed Al‐Helal; Neil G. Berry; Alexandre S. Lawrenson; Raman Sharma; Alison E. Shone; Stephen A. Ward; Giancarlo A. Biagini; Paul M. O’Neill
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