Tools
Tools
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: https://orcid.org/0000-0003-2331-3192, Biagini, Giancarlo ORCID: https://orcid.org/0000-0001-6356-6595 and O'Neill, Paul
(2015)
'2-Pyridylquinolone antimalarials with improved antimalarial activity and physicochemical properties'. MedChemComm, Vol 6, Issue 7, pp. 1252-1259.
|
Text
MedChemComm_2-Pyridylquinolone Antimalarials.pdf - Accepted Version Available under License Creative Commons Attribution. Download (700kB) | Preview |
Abstract
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): | https://doi.org/10.1039/c5md00062a |
| Related URLs: | |
| SWORD Depositor: | JISC Pubrouter |
| Depositing User: | Stacy Murtagh |
| Date Deposited: | 20 Nov 2017 17:04 |
| Last Modified: | 20 Nov 2017 17:04 |
| URI: | https://archive.lstmed.ac.uk/id/eprint/7845 |
Statistics
Actions (login required)
 |
Edit Item |