5-Substituted 3-chlorokenpaullone derivatives are potent inhibitors of Trypanosoma brucei bloodstream forms.

Abstract : Trypanothione synthetase is an essential enzyme for kinetoplastid parasites which cause highly disabling and fatal diseases in humans and animals. Inspired by the observation that N(5)-substituted paullones inhibit the trypanothione synthetase from the related parasite Leishmania infantum, we designed and synthesized a series of new derivatives. Although none of the new compounds displayed strong inhibition of Trypanosoma brucei trypanothione synthetase, several of them caused a remarkable growth inhibition of cultivated Trypanosoma brucei bloodstream forms. The most potent congener 3a showed antitrypanosomal activity in double digit nanomolar concentrations and a selectivity index of three orders of magnitude versus murine macrophage cells.
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Bioorganic & medicinal chemistry, Elsevier, 2016, 24 (16), pp.3790-800. 〈10.1016/j.bmc.2016.06.023〉
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Soumis le : lundi 9 octobre 2017 - 21:00:43
Dernière modification le : mercredi 21 février 2018 - 17:10:02

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Oliver Orban, Ricarda S Korn, Diego Benítez, Andrea Medeiros, Lutz Preu, et al.. 5-Substituted 3-chlorokenpaullone derivatives are potent inhibitors of Trypanosoma brucei bloodstream forms.. Bioorganic & medicinal chemistry, Elsevier, 2016, 24 (16), pp.3790-800. 〈10.1016/j.bmc.2016.06.023〉. 〈pasteur-01499026〉

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