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Isolation of F1-ATPase from the Parasitic Protist Trypanosoma brucei
Published on: January 22, 2019
Cell permeation of a Trypanosoma brucei aldolase inhibitor: evaluation of different enzyme-labile phosphate
Laurent Azéma1, Christian Lherbet, Cécile Baudoin
1Laboratoire SPCMIB, Groupe de Chimie Organique Biologique, Université Paul Sabatier UMR CNRS 5068, 118 route de Narbonne, 31062 Toulouse Cedex 4, France.
Bioorganic & Medicinal Chemistry Letters
|April 25, 2006
Abstract:
A series of four prodrugs directed against Trypanosoma brucei aldolase bearing various transient enzyme-labile phosphate protecting groups was developed. Herein, we describe the synthesis and evaluation of cell permeation of these prodrugs. The oxymethyl derivative was the most efficient prodrug with a good recovering of the free drug (IC(50)=20 microM) and without any measurable cytotoxicity.
