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, Texas Agricultural and Mechanical University (TAMU), and University of North Carolina (UNC), 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