OSF Preprints
Fluoro-methoxy-phenyl-substituted N-sulfonylpiperidine-mono-spiro-1,2,4,5-tetraoxanes as Multispecies-targeting Molecules
By Mohit Kumar Tiwari, Paweł Bakun, Emma Forest and 9 others.
Abstract
A novel series of heterocyclic fluoro-methoxy-phenyl-substituted N-sulfonylpiperidine mono-spiro-1,2,4,5-tetraoxanes was synthesised under metal-free, environmentally benign conditions. The compounds were evaluated against Plasmodium falciparum, Trypanosoma brucei, Mycobacterium, and cancer cell lines, showing micromolar antiparasitic and antimycobacterial activities with acceptable cytotoxicity. The synthesised derivatives exhibited activity against chloroquine-resistant P. falciparum strains. Selected compounds showed no lethality in Danio rerio larvae within the tested concentration range. Notably, the most promising analogue demonstrated multispecies-targeting activity against P. falciparum, T. brucei, and M. tuberculosis.






