Identification of new, effective and selective trypanocidal agents. Twelve novel acetohydroxamic acid derivatives based on 2-alkyl-2-aryl-2,6-diketopiperazine scaffolds have been synthesized and evaluated for their growth inhibitory activity against bloodstream form . All the analogs were remarkably potent inhibitors, with low micromolar to submicromolar activities. Structure-activity relationship studies demonstrated that the presence of an alkyl substituent at the (4)-position of the 2,6-diketopiperazine ring portion was, in general, beneficial to trypanocidal activity in this series. The highest activity resulted from the introduction of a methyl, -propyl or -butyl substituent to the (4)-position of the parent compound. Importantly, the most potent analogs were found to be highly selective against with respect to mammalian cells.
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