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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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https://hal-riip.archives-ouvertes.fr/pasteur-01499026
Contributor : Mariella Botta <>
Submitted on : Monday, October 9, 2017 - 9:00:43 PM
Last modification on : Sunday, December 1, 2019 - 4:44:08 PM

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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 and Medicinal Chemistry, Elsevier, 2016, 24 (16), pp.3790-800. ⟨10.1016/j.bmc.2016.06.023⟩. ⟨pasteur-01499026⟩

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