Abstract
Quaternized triflupromazine derivatives (QTDs) must possess benzyl groups attached to the quaternary nitrogen in order to have significant antitubercular potency. Replacing the quaternary amine with a triazole abolishes antitubercular activity. A modest halogen substitution effect exists, with the 4-bromophenyl QTD 3 having the best selectivity index (>21). All N-benzyl QTDs 1–4 similarly inhibit non-replicating, persistent Mycobacterium tuberculosis with MIC<8μM, and compounds 1–3 were all nontoxic to mammalian cells in vitro (IC50>128μM).
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