735283-86-0Relevant academic research and scientific papers
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
INDOLE ACETAMIDES AS INHIBITORS OF THE HEPATITIS C VIRUS NS5B POLYMERASE
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Page 52, (2010/02/08)
The present invention relates to indole and azaindole compounds of formula (I): wherein X1, X2, X3, X4, A1, Ar1, R1, R2 and n are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.
