Identification of heteroarylenamines as a new class of antituberculosis lead molecules |
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| Authors: | Copp Brent R Christiansen Holly C Lindsay Brent S G Franzblau Scott |
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| Institution: | Department of Chemistry, The University of Auckland, Private Bag 92019, Auckland, New Zealand. b.copp@auckland.ac.nz |
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| 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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