DNA Binding Affinity of Bisguanidine and Bis(2-aminoimidazoline) Derivatives with in Vivo Antitrypanosomal Activity

Journal of Medicinal Chemistry
2006.0

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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