Molecules (Basel, Switzerland) · 2021
Antimalarial Inhibitors Targeting Epigenetics or Mitochondria in Plasmodium falciparum: Recent Survey upon Synthesis and Biological Evaluation of Potential Drugs against Malaria.
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Koumpoura Christina L, Robert Anne, Athanassopoulos Constantinos M, Baltas Michel
Аннотация
Despite many efforts, malaria remains among the most problematic infectious diseases worldwide, mainly due to the development of drug resistance by P. falciparum. Over the past decade, new essential pathways have been emerged to fight against malaria. Among them, epigenetic processes and mitochondrial metabolism appear to be important targets. This review will focus on recent evolutions concerning worldwide efforts to conceive, synthesize and evaluate new drug candidates interfering selectively and efficiently with these two targets and pathways. The focus will be on compounds/scaffolds that possess biological/pharmacophoric properties on DNA methyltransferases and HDAC's for epigenetics, and on cytochrome bc1 and dihydroorotate dehydrogenase for mitochondrion.
Предметные рубрики MeSH
AnimalsAntimalarialsDNADihydroorotate DehydrogenaseDrug DiscoveryDrug ResistanceEnzyme InhibitorsEpigenesis, GeneticHistone DeacetylasesHumansMalaria, FalciparumMethyltransferasesMitochondriaOxidoreductases Acting on CH-CH Group DonorsPlasmodium falciparumQuinazolinesSignal TransductionStructure-Activity Relationship