Activity of diimidazoline amides against African trypanosomiasis

[Display omitted] 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...

Full description

Saved in:
Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 24; no. 3; pp. 944 - 948
Main Authors Dong, Yuxiang, Wang, Xiaofang, Cal, Monica, Kaiser, Marcel, Vennerstrom, Jonathan L.
Format Journal Article
LanguageEnglish
Published OXFORD Elsevier Ltd 01.02.2014
Elsevier
Subjects
African trypanosomiasis
Amides - chemistry
Amides - pharmacology
Amides - therapeutic use
Animals
Chemistry
Chemistry, Medicinal
Chemistry, Organic
Diimidazoline
Disease Models, Animal
Humans
Imidazolines - chemistry
Imidazolines - therapeutic use
Life Sciences & Biomedicine
Mice
Molecular Structure
Pharmacology & Pharmacy
Physical Sciences
Science & Technology
Trypanocidal Agents - chemistry
Trypanocidal Agents - pharmacology
Trypanosoma - drug effects
Trypanosoma brucei rhodesiense
Trypanosomiasis, African - drug therapy
Diimidazoline
African trypanosomiasis
Trypanosoma brucei rhodesiense
MILD
TRYPANOCIDAL ACTION
DRUGS
AROMATIC DIAMIDINES
ANTIPROTOZOAL AGENTS
Online AccessGet full text

Cover

More Information
Summary:[Display omitted] 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.
Bibliography:NIH RePORTER
ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ObjectType-Article-2
ObjectType-Feature-1
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2013.12.064