Triphenylphosphonium (TPP)-Conjugated Quinolone Analogs Displayed Significantly Enhanced Fungicidal Activity Superior to Its Parent Molecule.

ABSTRACT: Although 1-hydroxy-4-quinolone derivatives, such as 2-heptyl-4-hydroxyquinoline-N-oxide (HQNO), aurachin C, and floxacrine, have been reported as effective cytochrome bc₁ complex inhibitors, the bioactivity of these products is not ideal, presumably due to their low bioavailability in tissues, particularly their poor solubility and low mitochondrial accumulation. In order to overcome the drawbacks of these compounds and develop their use as agricultural fungicides acting by cytochrome bc₁ inhibition, in this study, three novel mitochondria-targeting quinolone analogs (mitoQNOs) were designed and synthesized by conjugating triphenylphosphonium (TPP) with quinolone. They exhibited greatly enhanced fungicidal activity compared to the parent molecule, especi

SUBMITTER: Wang J 

PROVIDER: S-EPMC10305039 | biostudies-literature | 2023 Jun

REPOSITORIES: biostudies-literature