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2-Pyridylquinolone antimalarials with improved antimalarial activity and physicochemical properties

Charoensutthivarakul, Sitthivut, David Hong, W., Leung, Suet C., Gibbons, Peter D., Bedingfield, Paul, Nixon, Gemma L., Lawrenson, Alexandre S., Berry, Neil G., Ward, Steve ORCID:, Biagini, Giancarlo ORCID: and O'Neill, Paul (2015) '2-Pyridylquinolone antimalarials with improved antimalarial activity and physicochemical properties'. MedChemComm, Vol 6, Issue 7, pp. 1252-1259.

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A series of 2-pyridylquinolones has been prepared in 5–7 steps and through lead optimisation, antimalarial activity as low as 12 nM against Plasmodium falciparum (Pf) has been achieved. Compared with previous analogues in this series, selected molecules have improved solubility, a reduced potential for off-target toxicity and improved metabolic stability profiles. Docking studies performed with a homology model of the Pfbc1 complex target demonstrate a key role for the Tyr16 residues in the recognition of highly active quinolone based inhibitors

Item Type: Article
Subjects: QV Pharmacology > Anti-Inflammatory Agents. Anti-Infective Agents. Antineoplastic Agents > QV 256 Antimalarials
QW Microbiology and Immunology > QW 52 Physiology and chemistry of microorganisms. Metabolism.
QX Parasitology > Protozoa > QX 135 Plasmodia
WC Communicable Diseases > Tropical and Parasitic Diseases > WC 750 Malaria
Faculty: Department: Biological Sciences > Department of Tropical Disease Biology
Digital Object Identifer (DOI):
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SWORD Depositor: JISC Pubrouter
Depositing User: Stacy Murtagh
Date Deposited: 20 Nov 2017 17:04
Last Modified: 20 Nov 2017 17:04


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