Novel alkylpolyaminoguanidines and alkylpolyaminobiguanides with potent antitrypanosomal activity.

Bioorganic & Medicinal Chemistry Letters
Xiangdong BiPatrick M Woster

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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Citations

Feb 13, 2008·In Vitro Cellular & Developmental Biology. Animal·Gen-Bao ShaoAi-Hua Gong
Jun 11, 2011·Chemical Reviews·Daniele CastagnoloMaurizio Botta
Jun 24, 2010·Journal of Medicinal Chemistry·Shiv K SharmaPatrick M Woster
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