AI Article Synopsis
- Recent research suggests that Ivermectin (IVM) may be effective in controlling malaria, prompting the development of new hybrid molecules that enhance its effectiveness by modifying its structure.* -
- The new hybrids, which maintain certain sugar components and incorporate features from IVM metabolites, were tested and found to be more effective against the blood stage of malaria than IVM itself.* -
- Some hybrid compounds also retained IVM's insecticidal properties, highlighting the importance of sugar moieties in maintaining this activity and aiding in the design of future IVM derivatives.*
Article Abstract
Preclinical and/or clinical studies have demonstrated the potential of Ivermectin (IVM) for malaria control. In order to improve its antiplasmodial activity and build on previous knowledge, we have designed a third generation of hybrid molecules in which selected pharmacophores were appended to the IVM macrolide, while retaining one or both sugar moieties at the C-13 position. Moreover, we synthesized IVM hybrids that contain structural features of potent IVM metabolites. The evaluation of the antiplasmodial activity of these compounds against pre-erythrocytic stages and erythrocytic stages identified molecules that displayed enhanced activity against the latter when compared to IVM. Additionally, two IVM intermediates and one IVM hybrid retained the insecticidal activity of the parental molecule, clarifying the contribution of the sugar moieties to this feature. Altogether, these results provide key structure-activity relationships to guide the rational design of new generations of IVM hybrids.
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Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC11613448 | PMC |
| http://dx.doi.org/10.1021/acs.jmedchem.4c01606 | DOI Listing |
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