123518-00-3Relevant academic research and scientific papers
Structure-activity relationship study of prion inhibition by 2-aminopyridine-3,5-dicarbonitrile-based compounds: Parallel synthesis, bioactivity, and in vitro pharmacokinetics
May, Barnaby C. H.,Zorn, Julie A.,Witkop, Juanita,Sherrill, John,Wallace, Andrew C.,Legname, Giuseppe,Prusiner, Stanley B.,Cohen, Fred E.
, p. 65 - 73 (2007/10/03)
2-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.
NOVEL HETEROCYCLIC COMPOUNDS AS IKK2 INHIBITORS WITH ANTI-HBV ACTIVITY
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Page/Page column 16-17, (2008/06/13)
This application relates to novel thienopyridines of Formula (I), which are IKK inhibitors and are useful for treating Hepatitis B infection and other diseases. This application also relates to pharmaceutical compositions comprising thienopyridines and the use of such compositions to treat Hepatitis B and other diseases.
CYCLIZATION OF NITRILES. XXX. SYNTHESIS, STRUCTURE, AND PROPERTIES OF 6-AMINO-4-ARYL(HETEROARYL)-3,5-DICYANO-2(1H)-PYRIDINETHIONES
Sharanin, Yu. A.,Promomenkov, V. N.,Shestopalov, A. M.,Nestorov, V. N.,Malenchuk, S. N.,et al.
, p. 560 - 565 (2007/10/02)
The reactions of arylmethylenecyanothioacetamides with malononitrile and of arylmethylenemalononitriles with cyanothioacetamide take place regioselectively with the formation of 6-amino-4-aryl-3,5-dicyano-2(1H)-pyridinethiones and not 5-arylmethylene-4,6-diamino-3-cyanopyridine-2-thiones.The 6-amino-4-aryl-3,5-dicyano-2(1H)-pyridinethiones are formed by the recyclization of the 4-aryl-2,6-diamino-3,5-dicyano-4H-thiopyranes.
