Description
New narrow-spectrum antibiotic against mycobacteria (tricyclic spirolactams (TriSLa compounds)), (Mycobacterium tuberculosis, abscessus, avium)
Achievements:
•200 CMI-synthesized anti-tuberculosis analogs: 10 nM
•Active against treatment-resistant non-replicating tuberculosis
•Specific inhibitor of electron transport in Mycobacterium (image)
•No cytotoxicity
Pharmacokinetics/ADME Properties:
•400 < MW < 550 g.mol⁻¹ ; 3,5 < LogD < 5, grande solubilité
•Stable sur le plan chimique et métabolique
•Demi-vie in vivo > 6 h ; Cmax > 10 µM, accumulation dans les poumons
•POC in vivo faite sur poissons zèbres infectés par M. marinum
Acts on the respiratory chain of mycobacteria
Blocks ATP production
Disrupts the balance of the NADH cofactor
In progress: In vivo proof of concept in mice
IP: Priority date: June 7, 2022