Molecular design, synthesis and biological evaluation of 1,4-dihydro-4-oxoquinoline ribonucleosides as TcGAPDH inhibitors with trypanocidal activity.

Fabyana A Soares,Renata Sesti-Costa,João Santana da Silva,Maria Cecília B V de Souza,Vitor F Ferreira,Fernanda da C Santos,Patricia A U Monteiro,Andrei Leitão,Carlos A Montanari

Bioorganic & Medicinal Chemistry Letters（2013）

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摘要

Neq135 is the first low micromolar trypanosomatidae inhibitor acting against Trypanosoma cruzi glyceraldehyde 3-phosphate dehydrogenase (TcGAPDH). It binds to the NAD+ site, being selective in vitro toward the parasite.

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关键词

Chagas disease,Trypanosoma cruzi,GAPDH,Isothermal titration calorimetry

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