© WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
Editor-in-Chief: Natalia Ortúzar
Impact Factor: 3.046
ISI Journal Citation Reports © Ranking: 2013: 18/58 (Chemistry Medicinal); 75/256 (Pharmacology & Pharmacy)
Online ISSN: 1860-7187
January 25, 2011
VIP: Pyrido[1,2-a]benzimidazole-Based Agents Active Against TB, MDR-TB, and XDR-TB
Marco Pieroni, Suresh K. Tipparaju, Shichun Lun, Yang Song, A. Willem Sturm, William R. Bishai, and Alan P. Kozikowski*
The tuberculosis (TB) drug pipeline is going dry; can we find new agents for treating TB and drug-resistant TB?
The total number of TB cases and deaths worldwide continues to increase, and current estimates are that 5% of the 9 million new cases anticipated in 2011 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. In an attempt to identify new therapeutics, the medicinal chemistry group at the University of Illinois at Chicago (USA), directed by Prof. Alan Kozikowski, has taken the lead in investigating a series of hit compounds obtained from the high-throughput screening of a chemical library of about 6000 drug-like molecules. His group, together with the research groups of Prof. William Bishai at Johns Hopkins University (Baltimore, MD, USA) and Prof. 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.
Received November 16, 2010; published online January 21, 2011, DOI: 10.1002/cmdc.201000490.