871930-30-2Relevant articles and documents
Development of safe one-pot synthesis of N-1- and C-2-substituted benzimidazole via reductive cyclization of o-nitroarylamine using Na 2S2O4
Oda, Shinichi,Shimizu, Hideki,Aoyama, Yasunori,Ueki, Tatsuo,Shimizu, Sumio,Osato, Hiroshi,Takeuchi, Yoshiyuki
, p. 96 - 101 (2012/05/31)
We report that the reductive cyclization of o-nitroarylamine with aldehyde using sodium dithionite (Na2S2O4) could be accelerated by addition of H2O, which made it possible to control the heat release of the reaction by semibatch-type operation. Safety evaluation was performed using DSC, ARSST, in situ IR analysis, and Multimax.
Non-nucleoside benzimidazole-based allosteric inhibitors of the hepatitis C virus NS5B polymerase: Inhibition of subgenomic hepatitis C virus RNA replicons in huh-7 cells
Beaulieu, Pierre L.,Bousquet, Yves,Gauthier, Jean,Gillard, James,Marquis, Martin,McKercher, Ginette,Pellerin, Charles,Valois, Serge,Kukolj, George
, p. 6884 - 6892 (2007/10/03)
A previously disclosed series of non-nucleoside allosteric inhibitors of the NS5B polymerase of the hepatitis C virus (HCV) was optimized to yield novel compounds with improved physicochemical properties and activity in cell-based assays. Replacement of ionizable carboxylic acids with neutral substituents in lead compounds produced inhibitors with cellular permeability and antiviral activity in a cell-based assay of subgenomic HCV RNA replication (replicon EC50 as low as 1.7 μM. The improvement in potency in this ex vivo model of HCV RNA replication validates, in part, the mechanism by which this class of allosteric benzimidazole derivatives inhibits the polymerase and represents a significant step forward in the discovery of novel HCV therapeutics.
