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Inhibition of trypanothione reductase by substrate analogues
E A Garrard1, E C Borman, B N Cook
1Department of Chemistry, Carleton College, Northfield, Minnesota 55057, USA.
Organic Letters
|November 14, 2000
Abstract:
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 K(i) values ranging from 30 to 91 microM.