The global number of tuberculosis (TB) cases and deaths continues to increase, and current estimates are that 5 % of the 9 million new cases anticipated this year will be due to multidrug-resistant (MDR) TB strains. Despite increasing attention to drug discovery for new anti-TB drugs, the pipeline of candidates is sparse.
To help identify new therapeutics, Alan Kozikowski’s medicinal chemistry group at the University of Illinois at Chicago, USA, has investigated a series of hit compounds obtained by screening a chemical library of ~6000 drug-like molecules. His group, together with the research groups of William Bishai at Johns Hopkins University, Baltimore, MD, USA, and Willem Sturm at the University of KwaZulu Natal, South Africa, were able to identify improved derivatives that have little cellular cytotoxicity. One of the best members of this novel class of anti-TB agents has activity similar to that of the first-line drugs currently used in therapy and, more importantly, this agent is active against several drug-resistant TB strains.
Image: (c) Wiley-VCH
- Pyrido[1,2-a]benzimidazole-Based Agents Active Against Tuberculosis (TB), Multidrug-Resistant (MDR) TB and Extensively Drug-Resistant (XDR) TB
M. Pieroni, S. K. Tipparaju, S. Lun, Y. Song, A. W. Sturm, W. R. Bishai, A. P. Kozikowski,
ChemMedChem 2011, 6(02).