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Drug development

Newly identified compound could both treat and prevent malaria

Bicyclic azetidines have the potential to both cure malaria and prevent malaria transmission, study shows.

X-ray crystal structure of the BRD7929 compound

Source: Kato N, Corner E, Sakata-Kato T, et al.

Bicyclic azetidines (pictured) induced a single-dose cure for malaria in mice 

The majority of current antimalarial drugs only target one stage of the parasite life cycle, and are threatened by the emergence of resistance. 

To discover new compounds with activity throughout the parasite life cycle, researchers screened 100,000 synthetic compounds with a broad range of 3D features, against a multidrug-resistant strain of the malaria parasite Plasmodium falciparum

The screen highlighted a family of compounds called the bicyclic azetidines. The researchers showed that two compounds in this family could induce a single-dose cure for malaria in mouse models. And one of the compounds, termed BRD7929, was able to eliminate blood parasites at all stages of the life cycle. 

Reporting in Nature (online, 7 September 2016)[1], the researchers say the findings show that bicyclic azetidines have the potential to both cure malaria and prevent malaria transmission, and may also be useful for prophylaxis in high-risk populations.

 

Researchers Nobutaka Kato (left) and Eamon Comer

Courtesy of Nobutaka Kato and Eamon Comer

Researchers Nobutaka Kato (left) and Eamon Comer at Harvard were two of the researchers who made the discovery

 

Citation: The Pharmaceutical Journal DOI: 10.1211/CP.2016.20201739

Readers' comments (2)

  • It will be very impressive to treat Malaria

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  • Why is this article so short??! can we have a bit more detail about how this new breakthrough actually works??? What part of the cycle does it affect? There have been some really brief articles published lately, it's really disappointing to see. I hope it's not going to continue...

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Supplementary images

  • X-ray crystal structure of the BRD7929 compound
  • Researchers Nobutaka Kato (left) and Eamon Comer at Harvard were two of the researchers who made the discovery

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