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Anti-Tuberculosis Compounds

Summary

Novel Mycobacterium tuberculosis thioredoxin reductase inhibitors with antimycobacterial activity in infected macrophages that overcomes problems of current anti-tuberculotics.

Technology Benefits

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

Technology Application

therapeutic development

Detailed Technology Description

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.

Type of Cooperation

Licensing

Application Date

22/06/2018 00:00:00

Application No.

WO2018EP66768 20180622

Classes

- international:
A61K31/47; A61K31/4709; A61P31/06; C07D215/44; C07D215/46; C07D401/12; C07D413/12
- cooperative:
C07D215/44; C07D215/46; C07D401/12; C07D413/12

Others

Patent application

ID No.

4941

Country/Region

Germany

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