Structure-Activity Relationship Refinement and Further Assessment of Indole-3-glyoxylamides as a Lead Series against Prion Disease

Structure–activity relationships within the indole‐3‐glyoxylamide series of antiprion agents have been explored further, resulting in discovery of several new compounds demonstrating excellent activity in a cell line model of prion disease (EC50

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Bibliographische Detailangaben
Veröffentlicht in:	ChemMedChem 2011-01, Vol.6 (1), p.115-130
Hauptverfasser:	Thompson, Mark J., Louth, Jennifer C., Ferrara, Steven, Sorrell, Fiona J., Irving, Benjamin J., Cochrane, Edward J., Meijer, Anthony J. H. M., Chen, Beining
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Cell Line drug discovery High-Throughput Screening Assays indoles Indoles - chemistry Kinetics Ligands medicinal chemistry Mice Models, Molecular prion disease Prion Diseases - drug therapy Prions - antagonists & inhibitors Prions - metabolism Protein Conformation Quantitative Structure-Activity Relationship Small Molecule Libraries - metabolism Small Molecule Libraries - pharmacology structure-activity relationships Sulfonylurea Compounds - chemistry
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Beschreibung
Zusammenfassung:	Structure–activity relationships within the indole‐3‐glyoxylamide series of antiprion agents have been explored further, resulting in discovery of several new compounds demonstrating excellent activity in a cell line model of prion disease (EC50
ISSN:	1860-7179 1860-7187
DOI:	10.1002/cmdc.201000383