Inhibition of trypanothione reductase by substrate analogues

Elizabeth A. Garrard, Emily C. Borman, Brian N. Cook, Emily J. Pike, David G. Alberg

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Abstract

(matrix presented) Trypanothione reductase (TR) catalyzes the NAPDH-dependent reduction of the spermidine-glutathione conjugate trypanothione, an antioxidant found in Trypanosomatid parasites. TR plays an essential role in the parasite's defense against oxidative stress and has emerged as a prime target for drug development. Here we report the synthesis of several trypanothione analogues and their inhibitory effects on T. cruzi TR. All are competitive inhibitors with Ki values ranging from 30 to 91 μM.

Original languageEnglish (US)
Pages (from-to)3639-3642
Number of pages4
JournalOrganic Letters
Volume2
Issue number23
DOIs
StatePublished - Nov 16 2000

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