Activity of diimidazoline amides against African trypanosomiasis

Yuxiang Dong; Xiaofang Wang; Monica Cal; Marcel Kaiser; Jonathan L. Vennerstrom

doi:10.1016/j.bmcl.2013.12.064

Activity of diimidazoline amides against African trypanosomiasis

Yuxiang Dong, Xiaofang Wang, Monica Cal, Marcel Kaiser, Jonathan L. Vennerstrom

Pharmaceutical Science

Research output: Contribution to journal › Article › peer-review

6 Scopus citations

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.

Original language	English (US)
Pages (from-to)	944-948
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	24
Issue number	3
DOIs	https://doi.org/10.1016/j.bmcl.2013.12.064
State	Published - Feb 1 2014

Keywords

African trypanosomiasis
Diimidazoline
Trypanosoma brucei rhodesiense

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/j.bmcl.2013.12.064

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title = "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.",

keywords = "African trypanosomiasis, Diimidazoline, Trypanosoma brucei rhodesiense",

author = "Yuxiang Dong and Xiaofang Wang and Monica Cal and Marcel Kaiser and Vennerstrom, {Jonathan L.}",

note = "Funding Information: This investigation received financial support from the NIH (1U01AI082051-01) and the Swiss Tropical and Public Health Institute. ",

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T1 - Activity of diimidazoline amides against African trypanosomiasis

AU - Dong, Yuxiang

AU - Wang, Xiaofang

AU - Cal, Monica

AU - Kaiser, Marcel

AU - Vennerstrom, Jonathan L.

N1 - Funding Information: This investigation received financial support from the NIH (1U01AI082051-01) and the Swiss Tropical and Public Health Institute.

PY - 2014/2/1

Y1 - 2014/2/1

N2 - 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.

AB - 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.

KW - African trypanosomiasis

KW - Diimidazoline

KW - Trypanosoma brucei rhodesiense

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JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 3

ER -

Activity of diimidazoline amides against African trypanosomiasis

Abstract

Keywords

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