9- and 11-substituted 4-azapaullones are potent and selective inhibitors of African trypanosoma
0301 basic medicine
0303 health sciences
Macrophages
Trypanosoma brucei brucei
Benzazepines
Trypanocidal Agents
Cell Line
3. Good health
Mice
Structure-Activity Relationship
03 medical and health sciences
Trypanosomiasis, African
Drug Design
Animals
Humans
Cell Proliferation
DOI:
10.1016/j.ejmech.2014.06.020
Publication Date:
2014-06-11T17:13:33Z
AUTHORS (12)
ABSTRACT
Trypanosomes from the "brucei" complex are pathogenic parasites endemic in sub-Saharan Africa and causative agents of severe diseases in humans and livestock. In order to identify new antitrypanosomal chemotypes against African trypanosomes, 4-azapaullones carrying α,β-unsaturated carbonyl chains in 9- or 11-position were synthesized employing a procedure with a Heck reaction as key step. Among the so prepared compounds, 5a and 5e proved to be potent antiparasitic agents with antitrypanosomal activity in the submicromolar range.
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CITATIONS (34)
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