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- Mendoza, Adela; Pérez-Silanes, Silvia; Quiliano, Miguel; Pabón, Adriana; Galiano, Silvia; González, Germán; Garavito, Giovanny; Zimic, Mirko; Vaisberg, Abraham; Aldana, Ignacio; Monge, Antonio; Deharo, Eric
- Experimental parasitology 2011 v.128 no.2 pp. 97-103
- Plasmodium berghei; Plasmodium falciparum; active sites; antimalarials; inhibitory concentration 50; mice; molecular models; parasites; parasitology; piperazine; plasmepsin; structure-activity relationships
- ... Piperazine and pyrrolidine derivatives were synthesised and evaluated for their capacity to inhibit the growth of Plasmodium falciparum chloroquine-resistant (FCR-3) strain in culture. The combined presence of a hydroxyl group, a propane chain and a fluor were shown to be crucial for the antiplasmodial activity. Five compounds of the aryl-alcohol series inhibited 50% of parasite growth at doses ⩽1 ...
- Moon, Sung-Ung; Kang, Jung-Mi; Kim, Tong-Soo; Kong, Yoon; Sohn, Woon-Mok; Na, Byoung-Kuk
- Experimental parasitology 2011 v.128 no.2 pp. 127-132
- Plasmodium falciparum; Plasmodium vivax; antimalarials; cysteine proteinases; hemoglobin; humans; hydrolysis; malaria; pH; parasites; parasitology; plasmepsin
- ... Plasmepsins, a family of aspartic proteases of Plasmodium species, are known to participate in a wide variety of cellular processes essential for parasite survival. Therefore, the plasmepsins of malaria parasites have been recognized as attractive antimalarial drug targets. Although the plasmepsins of P. falciparum have been extensively characterized, the plasmepsins of P. vivax are currently not ...