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. 2006 Jun 15;16(12):3229-32.
doi: 10.1016/j.bmcl.2006.03.048. Epub 2006 Apr 17.

Novel alkylpolyaminoguanidines and alkylpolyaminobiguanides with potent antitrypanosomal activity

Xiangdong Bi  1 , Christina Lopez, Cyrus J Bacchi, Donna Rattendi, Patrick M Woster
Affiliations

Novel alkylpolyaminoguanidines and alkylpolyaminobiguanides with potent antitrypanosomal activity

Xiangdong Bi et al. Bioorg Med Chem Lett. .

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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