DNA binding affinity of bisguanidine and bis(2-aminoimidazoline) derivatives with in vivo antitrypanosomal activity

摘要

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.