Novel alkylpolyaminoguanidines and alkylpolyaminobiguanides with potent antitrypanosomal activity

descriptionPublicationkeyboard_double_arrow_right Article 01 Jun 2006 English Publisher:Elsevier BVJournal:Bioorganic & Medicinal Chemistry Letters, volume 16, pages 3,229-3,232 (issn: 0960-894X,

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Authors: Xiangdong, Bi; Christina, Lopez; Cyrus J, Bacchi; Donna, Rattendi; Patrick M, Woster;

doi: 10.1016/j.bmcl.2006.03.048

pmid: 16616495

Novel alkylpolyaminoguanidines and alkylpolyaminobiguanides with potent antitrypanosomal activity

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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.

Related Organizations

Haskins Laboratories
United States
Wayne State College
United States
Wayne State University
United States
Pace University
United States

Keywords

Alkylation, Molecular Structure, Trypanosoma brucei brucei, Antiprotozoal Agents, Guanidines, Structure-Activity Relationship, Glutathione Reductase, Animals, Humans, NADH, NADPH Oxidoreductases

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