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

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. The 1,4-dihydro-4-oxoquinoline ribonucleoside, Neq135, is the first low micromol...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2013-08, Vol.23 (16), p.4597-4601
Hauptverfasser:	Soares, Fabyana A., Sesti-Costa, Renata, da Silva, João Santana, de Souza, Maria Cecília B.V., Ferreira, Vitor F., da C. Santos, Fernanda, Monteiro, Patricia A.U., Leitão, Andrei, Montanari, Carlos A.
Format:	Artikel
Sprache:	eng
Schlagworte:	4-Quinolones - chemical synthesis 4-Quinolones - chemistry 4-Quinolones - pharmacology Animals BALB 3T3 Cells calorimetry Chagas disease cytotoxicity Drug Design drugs fibroblasts Fibroblasts - drug effects GAPDH glyceraldehyde-3-phosphate dehydrogenase Glyceraldehyde-3-Phosphate Dehydrogenase (Phosphorylating) - antagonists & inhibitors hydrophobicity Inhibitory Concentration 50 Isothermal titration calorimetry Mice Nitroimidazoles - chemistry Nitroimidazoles - pharmacology ribonucleosides Ribonucleosides - chemical synthesis Ribonucleosides - chemistry Ribonucleosides - pharmacology spleen Structure-Activity Relationship titration Trypanocidal Agents - chemical synthesis Trypanocidal Agents - chemistry Trypanocidal Agents - pharmacology Trypanosoma cruzi Trypanosoma cruzi - drug effects Trypanosomatidae
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