- Guide to PHARMACOLOGY
Compound class: Synthetic organic
Comment: Compound 11c has been identified as a representative analogue for the 2-pyrazolyl quinolone series of antimalarial compounds .
The Malaria tab on this ligand page provides additional curator comments of relevance to the Guide to MALARIA PHARMACOLOGY.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
|Guide to Malaria Pharmacology Comments|
|The 2-pyrazolyl quinolone series has been designed and optimized for both potent antimalarial activity and improved drug metabolism and pharmacokinetic (DMPK) properties in vitro . Further preclinical studies are reported to be in progress, including an evaluation of activity against the liver and sexual blood stages of the parasite lifecycle.
Compound 11c is one of the structures claimed in patent WO2012069856 .
Potential Target/Mechanism Of Action: Compound 11c inhibits the Plasmodium mitochondrial cytochrome bc1 complex and is thought to bind to the Qi-site of cytochrome b .