735286-99-4Relevant academic research and scientific papers
Allosteric N-acetamide-indole-6-carboxylic acid thumb pocket 1 inhibitors of hepatitis C virus NS5B polymerase-Acylsulfonamides and acylsulfamides as carboxylic acid replacements
Beaulieu, Pierre L.,Coulombe, Rene,Gillard, James,Brochu, Christian,Duan, Jianmin,Garneau, Michel,Jolicoeur, Eric,Kuhn, Peter,Poupart, Marc-Andre,Rancourt, Jean,Stammers, Timothy A.,Thavonekham, Bounkham,Kukolj, George
, p. 66 - 81 (2013/03/14)
Acylsulfonamide and acylsulfamide as surrogates for the carboxylic acid function of N-acetamide-indole-6-carboxylic acids were evaluated as allosteric inhibitors of hepatitis C virus (HCV) NS5B polymerase. Several analogs displayed excellent antiviral pot
Finger-loop inhibitors of the HCV NS5b polymerase. Part 1: Discovery and optimization of novel 1,6- and 2,6-macrocyclic indole series
McGowan, David,Vendeville, Sandrine,Lin, Tse-I,Tahri, Abdellah,Hu, Lili,Cummings, Maxwell D.,Amssoms, Katie,Berke, Jan Martin,Canard, Maxime,Cleiren, Erna,Dehertogh, Pascale,Last, Stefaan,Fransen, Els,Van Der Helm, Elisabeth,Van Den Steen, Iris,Vijgen, Leen,Rouan, Marie-Claude,Fanning, Gregory,Nyanguile, Origène,Van Emelen, Kristof,Simmen, Kenneth,Raboisson, Pierre
scheme or table, p. 4431 - 4436 (2012/09/07)
Novel conformationaly constrained 1,6- and 2,6-macrocyclic HCV NS5b polymerase inhibitors, in which either the nitrogen or the phenyl ring in the C2 position of the central indole core is tethered to an acylsulfamide acid bioisostere, have been designed and tested for their anti-HCV potency. This transformational route toward non-zwitterionic finger loop-directed inhibitors led to the discovery of derivatives with improved cell potency and pharmacokinetic profile.
N-Acetamideindolecarboxylic acid allosteric 'finger-loop' inhibitors of the hepatitis C virus NS5B polymerase: discovery and initial optimization studies
Beaulieu, Pierre L.,Jolicoeur, Eric,Gillard, James,Brochu, Christian,Coulombe, Rene,Dansereau, Nathalie,Duan, Jianmin,Garneau, Michel,Jakalian, Araz,Kuehn, Peter,Lagace, Lisette,LaPlante, Steven,McKercher, Ginette,Perrault, Stephane,Poirier, Martin,Poupart, Marc-Andre,Stammers, Timothy,Thauvette, Louise,Thavonekham, Bounkham,Kukolj, George
scheme or table, p. 857 - 861 (2010/09/18)
SAR studies at the N1-position of allosteric indole-based HCV NS5B inhibitors has led to the discovery of acetamide derivatives with good cellular potency in subgenomic replicons (EC50 200 nM). This class of inhibitors displayed improved physicochemical properties and favorable ADME-PK profiles over previously described analogs in this class.
Development of carboxylic acid replacements in indole-N-acetamide inhibitors of hepatitis C virus NS5B polymerase
Stansfield, Ian,Pompei, Marco,Conte, Immacolata,Ercolani, Caterina,Migliaccio, Giovanni,Jairaj, Mark,Giuliano, Claudio,Rowley, Michael,Narjes, Frank
, p. 5143 - 5149 (2008/02/12)
Allosteric inhibition of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase enzyme has recently emerged as a viable strategy toward blocking replication of viral RNA in cell-based systems. We report here 2 series of indole-N-acetamides, bearing
Potent inhibitors of subgenomic hepatitis C virus RNA replication through optimization of indole-N-acetamide allosteric inhibitors of the viral NS5B polymerase
Harper, Steven,Avolio, Salvatore,Pacini, Barbara,Di Filippo, Marcello,Altamura, Sergio,Tomei, Licia,Paonessa, Giacomo,Di Marco, Stefania,Carfi, Andrea,Giuliano, Claudio,Padron, Julio,Bonelli, Fabio,Migliaccio, Giovanni,De Francesco, Raffaele,Laufer, Ralph,Rowley, Michael,Narjes, Frank
, p. 4547 - 4557 (2007/10/03)
Infections caused by hepatitis C virus (HCV) are a significant world health problem for which novel therapies are in urgent demand. Compounds that block replication of subgenomic HCV RNA in liver cells are of interest because of their demonstrated antivir
VIRAL POLYMERASE INHIBITORS
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Page 115, (2010/02/07)
An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula (I): wherein wherein A, B, R2, R3, L, M1, M2, M3, M4, Y1, Y0, Z and Sp are as defined in claim 1, or a salt thereof, as an inhibitor of HCV NS5B polymerase.
