Title of article
Novel alkylpolyaminoguanidines and alkylpolyaminobiguanides with potent antitrypanosomal activity
Author/Authors
Xiangdong Bi، نويسنده , , Christina Lopez، نويسنده , , Cyrus J. Bacchi، نويسنده , , Donna Rattendi، نويسنده , , Patrick M. Woster، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
4
From page
3229
To page
3232
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 μM, 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 μM, respectively. These agents represent a promising new class of potential antitrypanosomal agents.
Keywords
antiparasitic , Biguanide , guanidine , polyamine , Trypanothione , trypanosome , trypanosomiasis , trypanothione reductase , inhibitor
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796962
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