title: Identification of heteroarylenamines as a new class of antituberculosis lead molecules.
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.
authors: Department of Chemistry, The University of Auckland, Private Bag 92019, Auckland, New Zealand. b.copp@auckland.ac.nz
authors: Brent R
authors: BR
authors: Copp
authors: Holly C
authors: HC
authors: Christiansen
authors: Brent S
authors: BS
authors: Lindsay
authors: Scott
authors: S
authors: G Franzblau
mesh_terms: D000588:Amines / Q000737:chemistry* / Q000145:classification / Q000494:pharmacology*; D000995:Antitubercular Agents / Q000737:chemistry* / Q000145:classification* / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical; D004351:Drug Resistance; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000187:drug effects / Q000502:physiology; D013329:Structure-Activity Relationship
chemical_list: D000588:Amines; D000995:Antitubercular Agents