Antimalarial and β-hematin formation inhibitory activities of chromone derivatives
نویسندگان
چکیده
منابع مشابه
Antimalarial drugs inhibiting hemozoin (β-hematin) formation: A mechanistic update
Digestion of hemoglobin in the food vacuole of the malaria parasite produces very high quantities of redox active toxic free heme. Hemozoin (β-hematin) formation is a unique process adopted by Plasmodium sp. to detoxify free heme. Hemozoin formation is a validated target for most of the well-known existing antimalarial drugs and considered to be a suitable target to develop new antimalarials. H...
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malaria as one of the most recurrent infectious diseases caused by parasites of the genus plasmodium, kills several hundred thousand people especially in the tropical and subtropical regions of the world annually. terpenoids have served as the lead compounds to develop new antimalarial agents. the aromatic monoterpenoid, cuminaldehyde, isolated from the fruits of buniumpersicum was evaluated fo...
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Malaria and schistosomiasis are two of the most socioeconomically devastating parasitic diseases in tropical and subtropical countries. Since current chemotherapeutic options are limited and defective, there is an urgent need to develop novel antiplasmodials and antischistosomals. Hemozoin is a disposal product formed from the hemoglobin digestion by some blood-feeding parasites. Hemozoin forma...
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The hemolytic antimicrobial peptide dermaseptin S4 was recently shown to exert antimalarial activity. In this study, we attempted to understand the underlying mechanism(s) and identify derivatives with improved antimalarial activity. A number of dermaseptin S4 derivatives inhibited parasite growth with a 50% inhibitory concentration (IC(50)) in the micromolar range. Among these, the substituted...
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Pyronaridine, 2-methoxy-7-chloro-10[3',5'-bis(pyrrolidinyl-1-methyl-)4'hydroxyphenyl]aminobenzyl-(b)-1,5-naphthyridine, a new Mannich base schizontocide originally developed in China and structurally related to the aminoacridine drug quinacrine, is currently undergoing clinical testing. We now show that pyronaridine targets hematin, as demonstrated by its ability to inhibit in vitro beta-hemati...
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ژورنال
عنوان ژورنال: ScienceAsia
سال: 2019
ISSN: 1513-1874
DOI: 10.2306/scienceasia1513-1874.2019.45.221