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Discovery and Development of Highly Potent Inhibitors of Mycobacterium tuberculosis Growth In Vitro.


Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Apr 15 [updated 2013 Mar 7].

Author information

Southern Research Molecular Libraries Screening Center, Southern Research Institute, Birmingham, AL 35205
Center for Tuberculosis Research, Division of Infectious Diseases, Department of Medicine, Johns Hopkins University School of Medicine, Baltimore, MD 21231
University of Kansas Specialized Chemistry Center, University of Kansas, Lawrence, KS 66047
Department of Medicinal Chemistry, University of Kansas, Lawrence, KS 66047


Tuberculosis (TB) represents one of the top public health concerns worldwide. Over 2 billion people are infected with Mycobacterium tuberculosis (M. tb), the etiological agent of TB, resulting in 9.4 million new cases of active TB and 1.7 million deaths in 2009.1 The 1970s multidrug regimen for treating TB, recommended today by the WHO, has not been sufficient to eliminate TB in part due to the appearance of HIV/AIDS, failure of treatment programs, and enhanced transmission in hospitals and prisons. The recommended combination therapy for TB is lengthy and cumbersome since it can require medication of up to four drugs daily for 6–12 months. Limited healthcare system resources often lead to treatment interruption or failure, exacerbating drug resistance problems in places least capable of combating this disease. Thus, the discovery of new types of anti-tubercular drugs acting on novel drug targets with no cross-resistance to any existing drugs is urgently needed. Screening of ~330,000 compounds from the NIH Small Molecule Repository for their ability to inhibit the growth of M. tb identified a number of novel scaffolds with anti-tubercular activity. In this report, we discuss the development of one of those scaffolds leading to the probe ML242 (CID 2792221).

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