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Article

Mechanistic and biological characterisation of novelN5-substituted paullones targeting the biosynthesis of trypanothione inLeishmania

1 Jan 2020

Abstract excerpt

Trypanothione synthetase (TryS) produces N1,N8-bis(glutathionyl)spermidine (or trypanothione) at the expense of ATP. Trypanothione is a metabolite unique and essential for survival and drug-resistance of trypanosomatid parasites. In this study, we report the mechanistic and biological characterisation of optimised N5-substituted paullone analogues with anti-TryS activity. Several of the new derivatives retained...

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PMID: 32588679
DOI: 10.1080/14756366.2020.1780227

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