New Hope For Tuberculosis Treatment

  • Author: ChemViews
  • Published Date: 12 January 2012
  • Source / Publisher: ChemMedChem/Wiley-VCH
  • Copyright: WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
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Despite the availability of treatments for tuberculosis (TB), the threat this disease represents is still a painful reality for the ten million people infected and the two million that die each year. TB also represents an escalating threat to global health, with an increased prevalence of multidrug-resistant (MDR) TB strains, which are resistant to at least the two main first-line TB drugs isoniazid and rifampicin, and extremely drug-resistant (XDR) TB strains, which are also resistant to three or more of the six classes of second-line drugs.

Through a screening campaign, Lluís Ballell and colleagues, GlaxoSmithKline, Madrid, Spain, discovered two new families of closely related selective, non-cytotoxic, and potent antitubercular agents: thioquinolines and thiazoloquinolines. The compounds possess polysorbate (Tween) 80-dependent in vitro anti-mycobacterial activity..

A medicinal chemistry effort was then undertaken to generate lead-like structures to enable murine efficacy studies and help elucidate the in vivo implications of the in vitro observations. Although the final compounds showed only limited levels of systemic exposure in mice, modest levels of efficacy in vivo at nontoxic doses were observed.

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Magazine of Chemistry Europe (16 European Chemical Societies) published by Wiley-VCH