Incorporation of an Isohexide Subunit into the Endochin-like Quinolone Scaffold.

ABSTRACT: In order to improve the drug-likeness qualities, the antimalarial endochin-like quinolone (ELQ) scaffold has been modified by replacing the 4-(trifluoromethoxy)phenyl portion with an isoidide unit that is further adjustable by varying the distal O-substituents. As expected, the water solubilities of the new analogs are greatly improved, and the melting points are lower. However, the antimalarial potency of the new analogs is reduced to EC₅₀ > 1 millimolar, a result ascribable to the hydrophilic nature of the new substitution.

SUBMITTER: Senkina J 

PROVIDER: S-EPMC11314205 | biostudies-literature | 2024 Jul

REPOSITORIES: biostudies-literature