Polyamines with N-(3-phenylpropyl) substituents are effective competitive inhibitors of trypanothione reductase and trypanocidal agents

Add time:09/01/2019    Source:sciencedirect.com

Several N-(3-phenylpropyl)-substituted spermidine and spermine derivatives were prepared and found to be potent competitive inhibitors of Trypanosoma cruzi trypanothione reductase (seven compounds with Ki values <5 μM are described). The most effective inhibitor studied was compound 12 with a Ki value of 0.151 μM. Six of the compounds described are also effective trypanocides with IC50 values <1 μM.

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