Truncation of Samroiyotmycin: Tailored seco ‐Acids as Novel Antimalaria Compounds
Abstract
To facilitate synthetic access and address limitations associated with the tosyloxazole moiety in samroiyotmycin‐derived antimalarials, six truncated analogs were prepared in combination with C‐terminal methyl ester or carboxylic acid functionalities to mimic the electron‐poor character of the parent motif. Biological evaluation identified the 3,5‐bis(trifluoromethyl)phenyl‐substituted seco ‐acid as the most potent derivative, surpassing tosyl‐based reference compounds. The enhanced activity is consistent with a donor–acceptor interaction involving the electron‐deficient aryl unit and supports its proposed role in the inhibition of hemozoin formation.
Fields of Study & Subjects
Malaria Research and Control
Synthesis and Catalytic Reactions
Asymmetric Synthesis and Catalysis
Publication details
- Journal / source
- European Journal of Organic Chemistry
- Publisher
- Wiley
- Volume
- 29
- Issue
- 34
- Publication date
- 5 August 2026
- Language
- EN