Description
Achievements
•200 synthetized analogues à Anti-tuberculosis MIC - 10 nM
•Active on non-replicating drug tolerant tuberculosis
•Mycobacterium specific inhibitor of electron transport (image)
•No cytotoxicity
Pharmacokinetic/ADME properties:
- 400 < MW < 550 g.mol-1 ; 3.5 < LogD < 5, High solubility
- Chemically and metabolically stable
- In vivo t1/2 > 6 h; Cmax > 10 µM, accumulation in lungs
- In vivo POC established in M. marinum infected zebrafish