85598-51-2Relevant academic research and scientific papers
2-(2-Thienyl)-5,6-dihydroxy-4-carboxypyrimidines as inhibitors of the hepatitis C virus NS5B polymerase: Discovery, SAR, modeling, and mutagenesis
Koch, Uwe,Attenni, Barbara,Malancona, Savina,Colarusso, Stefania,Conte, Immacolata,Di Filippo, Marcello,Harper, Steven,Pacini, Barbara,Giomini, Claudia,Thomas, Steven,Incitti, Ilario,Tomei, Licia,De Francesco, Raffaele,Altamura, Sergio,Matassa, Victor G.,Narjes, Frank
, p. 1693 - 1705 (2007/10/03)
Infections caused by hepatitis C virus (HCV) are a significant world health problem for which novel therapies are in urgent demand. The polymerase of HCV is responsible for the replication of viral RNA. We recently disclosed dihydroxypyrimidine carboxylates 2 as novel, reversible inhibitors of the HCV NS5B polymerase. This series was further developed into 5,6-dihydroxy-2-(2- thienyl)pyrimidine-4-carboxylic acids such as 34 (EC50 9.3 μM), which now show activity in the cell-based HCV replication assay. The structure-activity relationship of these inhibitors is discussed in the context of their physicochemical properties and of the polymerase crystal structure. We also report the results of mutagenesis experiments which support the proposed binding model, which involves pyrophosphate-like chelation of the active site Mg ions.
Dihydroxypyrimidine carboxylic acids as viral polymerase inhibitors
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, (2008/06/13)
A class of 2-aryl-4,5-dihydroxy-6-carboxypyrimidines of formula (I): wherein Ar is an optionally substituted aryl or heterocyclic group; as well as compounds of formula (I) which are derivatised at one or more of the 4-hydroxy, 5-hydroxy or 6-carboxy groups; and tautomers thereof, and pharmaceutically acceptable salts or esters thereof; and inhibitors of viral polymerases, especially the hepatitis C virus (HCV) polymerase enzyme.
Palladium-Catalyzed Cyanation Reactions of Thiophene Halides
Erker, Thomas,Nemec, Stephanie
, p. 23 - 25 (2007/10/03)
The described method provides an efficient cyanation reaction of thiophene halides using tris(dibenzylidene-acetone)dipalladium(0), 1,1′-bis- (diphenylphosphino)ferrocene) and zinc powder as the catalyst system and Zn(CN)2 as the cyanide source
