89193-74-8Relevant academic research and scientific papers
Synthesis and antimalarial effects of phenothiazine inhibitors of a plasmodium falciparum cysteine protease
Domínguez, José N.,López, Simón,Charris, Jaime,Iarruso, Lúcido,Lobo, Gricela,Semenov, Andrey,Olson, Jed E.,Rosenthal, Philip J.
, p. 2726 - 2732 (2007/10/03)
Acridinediones have previously been shown to have potent antimalarial activity. A series of sulfur isosteres of acridinediones have been synthesized and evaluated for their inhibition of the Plasmodium falciparum cysteine protease falcipain and for their antimalarial activity. A number of these phenothiazines inhibited falcipain and demonstrated activity against cultured P. falciparum parasites at low micromolar concentrations. We propose that the compounds exerted their antimalarial effects by two mechanisms, one of which involves the inhibition of falcipain and a consequent block in parasite degradation of hemoglobin. Those compounds and related phenothiazines are worthy of further study as potential antimalarial agents.
