Novel Selective Inhibitors of the Zinc Plasmodial Aminopeptidase PfA-M1 as Potential Antimalarial Agents

Proteases that are expressed during the erythocytic stage of Plasmodium falciparum are newly explored drug targets for the treatment of malaria. We report here the discovery of potent inhibitors of PfA-M1, a metallo-aminopeptidase of the parasite. These compounds are based on a malonic hydroxamic te...

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Veröffentlicht in:	Journal of medicinal chemistry 2007-03, Vol.50 (6), p.1322-1334
Hauptverfasser:	Flipo, Marion, Beghyn, Terence, Leroux, Virginie, Florent, Isabelle, Deprez, Benoit P, Deprez-Poulain, Rebecca F
Format:	Artikel
Sprache:	eng
Schlagworte:	Aminopeptidases - antagonists & inhibitors Aminopeptidases - chemistry Animals Antibiotics. Antiinfectious agents. Antiparasitic agents Antimalarials - chemical synthesis Antimalarials - chemistry Antimalarials - pharmacology Antiparasitic agents Biochemistry Biochemistry, Molecular Biology Biodiversity Biological and medical sciences Cells, Cultured Cellular Biology Erythrocytes - drug effects Erythrocytes - parasitology Humans Hydroxamic Acids - chemical synthesis Hydroxamic Acids - chemistry Hydroxamic Acids - pharmacology Life Sciences Malonates - chemical synthesis Malonates - chemistry Malonates - pharmacology Medical sciences Metalloproteases - antagonists & inhibitors Metalloproteases - chemistry Microbiology and Parasitology Molecular biology Pharmacology. Drug treatments Plasmodium falciparum Plasmodium falciparum - drug effects Plasmodium falciparum - enzymology Protistology Quantitative Structure-Activity Relationship Solubility Systematics, Phylogenetics and taxonomy Zinc
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