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

DNA binding affinity of bisguanidine and bis(2-aminoimidazoline) derivatives with in vivo antitrypanosomal activity
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DOI:
10.1021/jm060295c
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发表时间:
2006-06-15
影响因子:
7.3
通讯作者:
Wilson, W. David
Wilson, W. David
中科院分区:
医学1区
文献类型:
--
作者:
Dardonville, Christophe;Barrett, Michael P.;Wilson, W. David

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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.