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- W1483993834 abstract "Bioorganometallics may represent an interesting strategy to solve the resistance problems of current antimalarial drugs. In an attempt to overcome these issues, ferroquine (FQ) was designed and synthesized. In parallel, its pharmacology properties were validated. Twenty years after, clinical trials of FQ have shown that this drug candidate is well tolerated and has a prominent role in the treatment of uncomplicated Plasmodium falciparum malaria. In the current context, understanding the mode(s) of action of effective antimalarial drugs is a key step in order to develop new drugs. New approaches to study the mechanism(s) of action of FQ were considered to elucidate the different aspects that confer the high antimalarial activity to this organometallic compound. For this purpose, the physicochemical properties in addition to its structural properties were studied. The studies highlight the importance of an intramolecular hydrogen bond and the influence of the iron atom upon the antimalarial activity of FQ. The accumulation and localization of FQ were studied through mass spectrometry and imaging experiments. Experimental and molecular modeling studies have explored the inhibition of the malarial pigment growth. The redox behavior of FQ was also considered in the oxidizing conditions mimicking the environment of the digestive vacuole of the parasite. The location of a specific hydroxyl radicals probe has highlighted the importance of the redox properties of the FQ in its antimalarial activity. In this chapter, the mechanism(s) of action of FQ will be reviewed and discussed in comparison with chloroquine, its purely organic parent drug." @default.
- W1483993834 created "2016-06-24" @default.
- W1483993834 creator A5041319437 @default.
- W1483993834 creator A5047671533 @default.
- W1483993834 date "2014-11-21" @default.
- W1483993834 modified "2023-09-30" @default.
- W1483993834 title "On the Molecular Mechanisms of the Antimalarial Action of Ferroquine" @default.
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- W1483993834 doi "https://doi.org/10.1002/9783527673438.ch05" @default.
- W1483993834 hasPublicationYear "2014" @default.
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