DESCRIPTION ELQ-300 is an orally active, 4(1H)-quinolone-based inhibitor of the malarial mitochondrial cytochrome bc1 complex . Structurally it is a derivative of endochin (PubChem CID 100474), which has potent antiplasmodial activity, but is highly metabolically unstable in mammals . Endochin blocks respiration in Plasmodium-infected red blood cells , and this mechanism of action was expoited for the development of novel 4(1H)-quinolone derivatives such as ELQ-300. ELQ-300 was tested in preclinical experiments and was found to be active against P. falciparum and P. vivax at all of the parasite life cycle stages that are important for the transmission of malaria.

Potential Target/Mechanism Of Action: ELQ-300 is an inhibitor of the malarial mitochondrial cytochrome bc1 complex that is active in vitro and in in vivo models of parasite transmission, which suggests that it has potential for both the treatment and prevention of malaria.

DESCRIPTION ELQ-300 is a late lead candidate from a novel class of 4(1H)-quinolone-based compounds with potent antimalarial activity . The ELQs (endochin-like quinolones) are structural derivatives of endochin (PubChem CID 100474), which has potent antiplasmodial activity, but is highly metabolically unstable in mammals .

The Malaria tab on this ligand page provides additional curator comments of relevance to the Guide to MALARIA PHARMACOLOGY. (GtoPdb)

DESCRIPTION ELQ-300 is a potent and orally bioavailable antimalarial agent, and it is a novel inhibitor of the reductive (Qi) site of the cytochrome bc1 complex (complex III in the electron transport chain). (BOC Sciences Bioactive Compounds)