In Vitro and In Vivo Inhibition of the Mycobacterium tuberculosis
- 11 February 2022
- Resource Type: Anti-Infectives, Articles & Whitepapers, Medicinal Chemistry
Learn more about fighting tuberculosis by targeting the essential enzyme PptT.
Together with collaborators at Weill Cornell Medical College, we identified the amidinourea compound AU8918, through a phenotypic screen, as an interesting anti-TB compound. We went on to identify its target within Mycobacterium tuberculosis, as phosphopantetheinyl transferase (PptT) – an essential enzyme involved in synthesis of cellular lipids and virulence factors.
This paper describes:
- Next steps taken in further pursuit of this novel anti-TB series
- An expanded collaboration within the TB Drug Accelerator consortium
- Latest structure guided SAR exploration around AU8918 for more potent and safest Lead-like analogs