53369-77-0Relevant academic research and scientific papers
Design, Synthesis, and Evaluation of Novel Ferroquine and Phenylequine Analogues as Potential Antiplasmodial Agents
Jacobs, Leon,De Kock, Carmen,De Villiers, Katherine A.,Smith, Peter J.,Smith, Vincent J.,Van Otterlo, Willem A. L.,Blackie, Margaret A. L.
, p. 2099 - 2110 (2015/12/23)
7-Chloroquinoline-based antimalarial drugs are effective in the inhibition of hemozoin formation in the food vacuole of the Plasmodium parasite, the causative agent of malaria. We synthesized five series of ferroquine (FQ) and phenylequine (PQ) derivatives, which display good in vitro efficacy toward both the chloroquine-sensitive (CQS) NF54 (IC50: 4.2 nm) and chloroquine-resistant (CQR) Dd2 (IC50: 33.7 nm) strains of P. falciparum. Several compounds were found to have good inhibitory activity against β-hematin formation in an NP-40 detergent assay, with IC50 values ranging between 10.4 and 19.2 μm.
Synthesis and evaluation of phenylequine for antimalarial activity in vitro and in vivo
Blackie, Margaret A.L.,Yardley, Vanessa,Chibale, Kelly
supporting information; experimental part, p. 1078 - 1080 (2010/06/19)
Synthesis of the potent antiplasmodial 4-aminoquinoline, phenylequine (PQ), is reported for the first time. PQ and the two analogues show increased efficacy in moving from the chloroquine sensitive D10 to the chloroquine resistant K1 strain in vitro. The
