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ID: ALA3286354
Journal: Eur J Med Chem
Title: 9- and 11-Substituted 4-azapaullones are potent and selective inhibitors of African trypanosoma.
Authors: Maiwald F, Benítez D, Charquero D, Dar MA, Erdmann H, Preu L, Koch O, Hölscher C, Loaëc N, Meijer L, Comini MA, Kunick C.
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.
CiteXplore: 24973661