Skip to Main content Skip to Navigation
New interface
Journal articles

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.
Document type :
Journal articles
Complete list of metadata

https://hal-riip.archives-ouvertes.fr/pasteur-01499026
Contributor : Mariella Botta Connect in order to contact the contributor
Submitted on : Monday, October 9, 2017 - 9:00:43 PM
Last modification on : Tuesday, January 18, 2022 - 2:50:08 PM

Identifiers

Collections

Citation

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

Share

Metrics

Record views

67