107582-20-7Relevant articles and documents
Non-nucleoside inhibitors of the hepatitis C virus NS5B polymerase: Discovery and preliminary SAR of benzimidazole derivatives
Beaulieu, Pierre L.,Boes, Michael,Bousquet, Yves,Fazal, Gulrez,Gauthier, Jean,Gillard, James,Goulet, Sylvie,LaPlante, Steven,Poupart, Marc-Andre,Lefebvre, Sylvain,McKercher, Ginette,Pellerin, Charles,Austel, Volkhard,Kukolj, George
, p. 119 - 124 (2004)
Benzimidazole 5-carboxamide derivatives from a combinatorial screening library were discovered as specific inhibitors of the NS5B polymerase of the hepatitis C virus (HCV). Initial hit-to-lead activities taking advantage of high-throughput parallel synthetic techniques, identified a 1,2-disubstituted benzimidazole 5-carboxylic acid scaffold as the minimum core for biological activity. Potent analogues in this series inhibit the polymerase at low micromolar concentrations and provide an attractive 'drug-like' lead structure for further optimization and the development of potential HCV therapeutics.
Regioselective C-H Azidation of Anilines and Application to Synthesis of Key Intermediate for Pharmaceutical
Seki, Masahiko,Takahashi, Yusuke
, p. 7842 - 7848 (2021/06/28)
A catalytic system for regioselective C-H azidation of inactive anilines was developed. In the presence of CuSO4·5H2O, simultaneous addition of NaN3 and Na2S2O8 to aq. CH3CN solution of free anilines under weakly acidic conditions (pH 4.5) smoothly underwent C-H azidation to provide corresponding α-azidated products in high yields. Methyl α-azidoanthranilate obtained by this method was readily transformed via simple reduction followed by cyclization to methyl 2-ethoxybenzimidazol-7-carboxylate, a key intermediate for antihypertensive Candesartan Cilexetil.
BIS(2-HALOACETAMIDO)-COMPOUNDS FOR USE AS LINKING AGENTS AND RESULTANT PRODUCTS WHICH COMPRISE ANTIBODIES, HALF-ANTIBODIES AND ANTIBODY FRAGMENTS
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Page/Page column 27; 30, (2021/01/23)
Bis(2-haloacetamido)- compounds for use as linkers to chemically cross-linking multiple thiol groups, and particularly, although not exclusively, the thiol groups of cysteine amino acids in peptide chains are described, along with their use as linking age
