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

AuthorsDardonville, Christophe ; Barrett, Michael P.; Brun, Reto; Kaiser, Marcel; Tanious, Farial; Wilson, W. David
Issue Date2006
PublisherAmerican Chemical Society
CitationJournal of Medicinal Chemistry 49 : 3748- 3752 (2006)
AbstractA 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.
Publisher version (URL)http://dx.doi.org/10.1021/jm060295c
Appears in Collections:(IQM) Artículos
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