Anti-Tuberculosis Compounds
Novel Mycobacterium tuberculosis thioredoxin reductase inhibitors with antimycobacterial activity in infected macrophages that overcomes problems of current anti-tuberculotics.
Novel class of compounds that inhibit a novel target with potential to overcome resistance problems of M. tuberculosis to other drugs
Viability of infected macrophages is not affected
Increased bioactivity by optimized permeability through the cell wall of M. tuberculosis
therapeutic development
The interaction between the mycobacterial thioredoxin reductase (TrxR) and its substrate thioredoxin (Trx) is a promising new drug target for the treatment of tuberculosis, since Mtb lacks the common glutathione system and the mycobacterial TrxR shows a substantial difference in sequence, mechanism and structure to human TrxRs. It was shown that TrxR is essential for thiol redox homeostasis and genetic inactivation in vivo eradicates Mtb during acute and chronic mouse infections. In order to further improve the bioactivity of promising compounds, researchershave focused on optimizing the physico-chemical properties that are important for permeability, since M. tuberculosis shows an unusual thick and impermeable cell wall.
Licensing
22/06/2018 00:00:00
WO2018EP66768 20180622
- international:
A61K31/47; A61K31/4709; A61P31/06; C07D215/44; C07D215/46; C07D401/12; C07D413/12
- cooperative:
C07D215/44; C07D215/46; C07D401/12; C07D413/12
Patent application
4941
德國
