نتایج جستجو برای: antimalarial agents
تعداد نتایج: 366169 فیلتر نتایج به سال:
Among the known antimalarial drugs, chloroquine (CQ) and other 4-aminoquinolines have shown high potency and good bioavailability. Yet complications associated with drug resistance necessitate the discovery of effective new antimalarial agents. ADMET prediction studies were employed to evaluate a library of new molecules based on the 4-aminoquinolone-related structure of CQ. Extensive in vitro ...
A series of alkylated (bis)urea and (bis)thiourea polyamine analogues were synthesized and screened for antimalarial activity against chloroquine-sensitive and -resistant strains of Plasmodium falciparum in vitro. All analogues showed growth inhibitory activity against P. falciparum at less than 3 μM, with the majority having effective IC(50) values in the 100-650 nM range. Analogues arrested...
Abstract: Malaria is a potentially fatal parasitic disease brought on by five Plasmodium species, including falciparum, vivax, ovale, malariae, and knowlesi. The fast emergence of P. falciparum resistance to currently available treatments has increased health concerns in developing countries. growth emphasizes the need for novel, secure, cost-effective antimalarial drug that can treat malaria r...
The increasing resistance of malaria parasites to antimalarial drugs is a major contributor to the reemergence of the disease as a major public health problem and its spread in new locations and populations. Among potential targets for new modes of chemotherapy are malarial proteases, which appear to mediate processes within the erythrocytic malarial life cycle, including the rupture and invasi...
The Plasmodium falciparum cysteine proteases falcipain-2 and falcipain-3 appear to be required for hemoglobin hydrolysis by intraerythrocytic malaria parasites. Previous studies showed that peptidyl vinyl sulfone inhibitors of falcipain-2 blocked the development of P. falciparum in culture and exerted antimalarial effects in vivo. We now report the structure-activity relationships for inhibitio...
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