AI Article Synopsis
- The drug arteflene (Ro 42-1611), which contains peroxide, produces an alkyl radical when its peroxide bond is broken in the presence of a heme model like Mn(II)(TPP).
- Researchers have successfully captured this alkyl radical using TEMPO and have analyzed the various products resulting from arteflene's activation.
- Findings indicate that under these experimental conditions, arteflene is less effective as an alkylating agent than artemisinin, which has a trioxane structure.
Article Abstract
The peroxide-containing antimalarial drug arteflene (Ro 42-1611) generates an alkyl radical after the reductive homolytic cleavage of the peroxide bond in the presence of a heme model Mn(II)(TPP). This alkyl radical has been trapped by TEMPO, and the different products of the reduction activation of arteflene have been characterized. These data suggest that, in these experimental conditions, arteflene is not a significant alkylating agent compared to artemisinin, a trioxane-containing antimalarial drug.
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Characterization of the Main Radical and Products Resulting from a Reductive Activation of the Antimalarial Arteflene (Ro 42-1611).
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Article Synopsis
- The drug arteflene (Ro 42-1611), which contains peroxide, produces an alkyl radical when its peroxide bond is broken in the presence of a heme model like Mn(II)(TPP).
- Researchers have successfully captured this alkyl radical using TEMPO and have analyzed the various products resulting from arteflene's activation.
- Findings indicate that under these experimental conditions, arteflene is less effective as an alkylating agent than artemisinin, which has a trioxane structure.
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