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Activity of diimidazoline amides against African trypanosomiasis.


ABSTRACT: We identified several diimidazoline mono- and diamides that were as potent as pentamidine against Trypanosoma brucei rhodesiense in vitro. All of these were also less cytotoxic than pentamidine, but none was as effective as the latter in a T. brucei rhodesiense-infected mouse model. A single imidazoline may be sufficient for high antitrypanosomal activity provided that a second weak base functional group is present.

SUBMITTER: Dong Y 

PROVIDER: S-EPMC3925368 | biostudies-literature | 2014 Feb

REPOSITORIES: biostudies-literature

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Activity of diimidazoline amides against African trypanosomiasis.

Dong Yuxiang Y   Wang Xiaofang X   Cal Monica M   Kaiser Marcel M   Vennerstrom Jonathan L JL  

Bioorganic & medicinal chemistry letters 20131222 3


We identified several diimidazoline mono- and diamides that were as potent as pentamidine against Trypanosoma brucei rhodesiense in vitro. All of these were also less cytotoxic than pentamidine, but none was as effective as the latter in a T. brucei rhodesiense-infected mouse model. A single imidazoline may be sufficient for high antitrypanosomal activity provided that a second weak base functional group is present. ...[more]

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