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Updated: Aug 9, 2026

A Direct, Early Stage Guanidinylation Protocol for the Synthesis of Complex Aminoguanidine-containing Natural Products
Published on: September 9, 2016
Novel alkylpolyaminoguanidines and alkylpolyaminobiguanides with potent antitrypanosomal activity
Xiangdong Bi1, Christina Lopez, Cyrus J Bacchi
1Department of Pharmaceutical Sciences, Wayne State University, 259 Mack Ave, Detroit, MI 48202, USA.
Abstract:
A series of polyaminoguanidines and polyaminobiguanides were synthesized and evaluated as potential antitrypanosomal agents. These analogues inhibit trypanothione reductase (TR) with IC50 values as low as 0.95 microM, but do not inhibit the closely related human enzyme glutathione reductase (GR). The most effective analogues, 7a, 7b and 8d, inhibited parasitic growth in vitro with IC50 values of 0.18, 0.09 and 0.18 microM, respectively. These agents represent a promising new class of potential antitrypanosomal agents.
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