2. Academic Validation
  3. Identification of heteroarylenamines as a new class of antituberculosis lead molecules

Identification of heteroarylenamines as a new class of antituberculosis lead molecules

  • Bioorg Med Chem Lett. 2005 Sep 15;15(18):4097-9. doi: 10.1016/j.bmcl.2005.06.010.
Brent R Copp 1,  Holly C Christiansen,  Brent S Lindsay,  Scott G Franzblau
Affiliations

Affiliation

  • 1 Department of Chemistry, The University of Auckland, Private Bag 92019, Auckland, New Zealand. [email protected]
PMID: 16005211 DOI: 10.1016/j.bmcl.2005.06.010
Abstract

Enamine-containing analogues of heteroarylquinones were prepared based on initial screening data observed against Mycobacterium tuberculosis H37Rv (Mtb). Several analogues showed moderate to good inhibitory activity, with one analogue (7) also demonstrating acceptable toxic selectivity (MIC 0.39 microg/mL, SI 15). Activity towards a range of single-drug-resistant strains of Mtb was suggestive of a novel mechanism of action for 7.

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