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English2-Aminopyridine-3,5-dicarbonitrile compounds were previously identified as mimetics of dominant-negative prion protein mutants and inhibit prion replication in cultured cells. Here, we report findings from a comprehensive structure-activity relationship study of the 6-aminopyridine-3,5-dicarbonitrile scaffold. We identify compounds with significantly improved bioactivity (approximately 40-fold) against replication of the infectious prion isoform (PrPSc) and suitable pharmacokinetic profiles to warrant evaluation in animal models of prion disease.
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http://hdl.handle.net/20.500.11767/14465| Titolo: | Structure-activity relationship study of prion inhibition by 2-aminopyridine-3,5-dicarbonitrile-based compounds: parallel synthesis, bioactivity, and in vitro pharmacokinetics |
| Autori: | MAY BC; ZORN JA; WITKOP J; SHERRILL J; WALLACE AC; LEGNAME G; PRUSINER SB; COHEN FE |
| Rivista: | JOURNAL OF MEDICINAL CHEMISTRY |
| Data di pubblicazione: | 2007 |
| Volume: | 50 |
| Fascicolo: | 1 |
| Pagina iniziale: | 65 |
| Pagina finale: | 73 |
| Digital Object Identifier (DOI): | 10.1021/jm061045z |
| Appare nelle tipologie: | 1.1 Journal article |
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