Literature DB >> 16616495

Novel alkylpolyaminoguanidines and alkylpolyaminobiguanides with potent antitrypanosomal activity.

Xiangdong Bi1, Christina Lopez, Cyrus J Bacchi, Donna Rattendi, Patrick 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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Year:  2006        PMID： 16616495     DOI： 10.1016/j.bmcl.2006.03.048

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  22 in total

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