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
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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