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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.
Structure-activity relationship study of prion inhibition by 2-aminopyridine-3,5-dicarbonitrile-based compounds: parallel synthesis, bioactivity, and in vitro pharmacokinetics / May, Bc; Zorn, Ja; Witkop, J; Sherrill, J; Wallace, Ac; Legname, Giuseppe; Prusiner, Sb; Cohen, Fe. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - 50:1(2007), pp. 65-73. [10.1021/jm061045z]
| 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, Giuseppe; Prusiner, Sb; Cohen, Fe | |
| Rivista: | ||
| Data di pubblicazione: | 2007 | |
| Volume: | 50 | |
| Fascicolo: | 1 | |
| Pagina iniziale: | 65 | |
| Pagina finale: | 73 | |
| Digital Object Identifier (DOI): | http://dx.doi.org/10.1021/jm061045z | |
| Appare nelle tipologie: | 1.1 Journal article |
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