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  • Title: DNA binding affinity of bisguanidine and bis(2-aminoimidazoline) derivatives with in vivo antitrypanosomal activity.
    Author: Dardonville C, Barrett MP, Brun R, Kaiser M, Tanious F, Wilson WD.
    Journal: J Med Chem; 2006 Jun 15; 49(12):3748-52. PubMed ID: 16759117.
    Abstract:
    A new antitrypanosomal hit compound that cures an acute (STIB 900) mouse model of Trypanosoma brucei rhodesiense trypanosomiasis is described. This bis(2-aminoimidazolinium) dicationic compound proved to be an excellent DNA minor groove binder, suggesting a possible mechanism for its trypanocidal activity. From these studies, the 4,4'-diaminodiphenylamine skeleton emerged as a good scaffold for antitrypanosomal drugs.
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