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Bioorg Med Chem Lett ; 15(18): 4097-9, 2005 Sep 15.
Article in English | MEDLINE | ID: mdl-16005211

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.


Subject(s)
Amines/chemistry , Amines/pharmacology , Antitubercular Agents/chemistry , Antitubercular Agents/classification , Amines/classification , Antitubercular Agents/pharmacology , Drug Evaluation, Preclinical , Drug Resistance , Inhibitory Concentration 50 , Molecular Structure , Mycobacterium tuberculosis/drug effects , Mycobacterium tuberculosis/physiology , Structure-Activity Relationship
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