Synthesis and biological evaluation of benzhydryl-based antiplasmodial agents possessing Plasmodium falciparum chloroquine resistance transporter (PfCRT) inhibitory activity
Relitti, Nicola; Federico, Stefano; Pozzetti, Luca; Butini, Stefania; Lamponi, Stefania; Taramelli, Donatella; D'Alessandro, Sarah; Martin, Rowena; Shafik, Sarah; Summers, Robert; Babij, Simone; Habluetzel, Annette; Tapanelli, Sofia; Caldelari, Reto; Gemma, Sandra; Campiani, Giuseppe
Due to the surge in resistance to common therapies, malaria remains a significant concern to human health worldwide. In chloroquine (CQ)-resistant (CQ-R) strains of Plasmodium falciparum, CQ and related drugs are effluxed from the parasite’s digestive vacuole (DV). This process is mediated by mutant isoforms of a protein called CQ resistance transporter (PfCRT). CQ-R strains can be partially re-sensitized to CQ by verapamil (VP), primaquine (PQ) and other compounds, and this has been shown to...[Show more]
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|Source:||European Journal of Medicinal Chemistry|
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