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Updated: Feb 15, 2026

Facile Synthesis of Worm-like Micelles by Visible Light Mediated Dispersion Polymerization Using Photoredox Catalyst

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Nuevos análogos de pretomanida antituberculosos como potentes cargas útiles en micelas poliméricas: Aprovechamiento

Andrew M Thompson¹, Nils-Jørgen K Dal², Francesca Boldrin³

¹Auckland Cancer Society Research Centre, School of Medical Sciences, The University of Auckland, Private Bag 92019, Auckland, 1142, New Zealand; Maurice Wilkins Centre for Molecular Biodiscovery, The University of Auckland, Private Bag 92019, Auckland, 1142, New Zealand.

European journal of medicinal chemistry

|February 13, 2026

Abstract:

Third-generation derivatives of the tuberculosis drug pretomanid featuring acetylene-bridged aryl-heteroaryl or heterotriaryl side chains were designed as novel agents for nanoparticle-based delivery, seeking better efficacy and safety. While all nitro compounds retained excellent activity against Mycobacterium tuberculosis, several examples in the latter class excelled as having potency superior to the original lead (7) but equivalent to or reduced lipophilicity, implying enhanced lipophilic efficiency. Initial studies suggested a similar mode of action against the related fish pathogen, M. marinum; therefore, fourteen candidates were further assessed as micellar formulations in M. marinum-infected zebrafish embryo assays. Overall, the best new analogue was 14 (the 6-amino-linked congener of 7), which was non-toxic and displayed efficacy comparable to 7 in both the blood and neural tube M. marinum infection models. Lead 14 also exhibited high microsomal stability, moderate cell permeability in an MDR1-MDCKII screen, and an enhanced pharmacokinetic profile in mice, with 93 % oral bioavailability.

Palabras clave:

Eficacia in vivo Nanopartícula Permeabilidad Farmacocinética Pretomanida Tuberculosis Pez cebra

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