نتایج جستجو برای: antimalarial compounds
تعداد نتایج: 232060 فیلتر نتایج به سال:
8-Arylinosines have been scarcely studied for therapeutic purposes, probably due to difficulties in their synthesis. The recently described direct arylation reaction at position 8 of purine nucleosides has been employed to synthesize a series of 8-aryl and 8-pyridylinosines. These compounds have been studied for hydrolytic stability and subjected to biological evaluation. Three compounds have s...
The apicomplexan parasites that cause malaria and babesiosis invade and proliferate within erythrocytes. To assess the potential for common antiparasitic treatments, we measured the sensitivities of multiple species of Plasmodium and Babesia parasites to the chemically diverse collection of antimalarial compounds in the Malaria Box library. We observed that these parasites share sensitivities t...
Members of the genus Leishmania are parasitic protozoans that infect about two million people per annum (5), and they are emerging as serious opportunistic infective agents in human immunodeficiency virus-infected patients (4). Malaria parasites are responsible for 1.5 to 2.7 million deaths annually, primarily in Africa (10). The effort to find new antimalarial agents is still a high priority g...
Molecular topology allows describing molecular structures following a two-dimensional approach by taking into account how the atoms are arranged internally through connection matrix between that part of structure. Various indices (unique for each molecule) can be determined, such as Zagreb, Balaban, and topological indices. These have been correlated with physical chemistry properties weight, b...
Malaria disease continues to be a major health problem worldwide due to the emergence of multidrug-resistant strains of Plasmodium falciparum. In recent days, artemisinin (ART)-based drugs and combination therapies remain the drugs of choice for resistant P. falciparum malaria. However, resistance to ART-based drugs has begun to appear in some parts of the world. Endoperoxide compounds (natural...
The apicoplast is an essential plastid organelle found in Plasmodium parasites which contains several clinically validated antimalarial-drug targets. A chemical rescue screen identified MMV-08138 from the "Malaria Box" library of growth-inhibitory antimalarial compounds as having specific activity against the apicoplast. MMV-08138 inhibition of blood-stage Plasmodium falciparum growth is stereo...
The efficacy of most marketed antimalarial drugs has been compromised by evolution of parasite resistance, underscoring an urgent need to find new drugs with new mechanisms of action. We have taken a high-throughput approach toward identifying novel antimalarial chemical inhibitors of prioritized drug targets for Plasmodium falciparum, excluding targets which are inhibited by currently used dru...
Health care in malaria endemic areas of Africa is at a crucial tipping point. On the positive side, increased commitment to and funding for malaria control is leading to improved access to effective antimalarial drugs, with over the counter availability and extensive subsidies. However, current efforts do not yet adequately address the need for tools to diagnose malaria accurately and track its...
BACKGROUND Malaria especially falciparum malaria still causes high morbidity and mortality in tropical countries. Several factors have been linked to this situation and the most important one is the rapid spread of parasite resistance to the currently available antimalarials, including artemisinin. Artemisinin is the main component of the currently recommended antimalarial, artemisinin based co...
Among promising new targets for antimalarial chemotherapy are the cysteine protease hemoglobinases falcipain-2 and falcipain-3. We evaluated the activities of synthetic peptidyl aldehyde and alpha-ketoamide cysteine protease inhibitors against these proteases, against cultured Plasmodium falciparum parasites, and in a murine malaria model. Optimized compounds inhibited falcipain-2 and falcipain...
نمودار تعداد نتایج جستجو در هر سال
با کلیک روی نمودار نتایج را به سال انتشار فیلتر کنید