5409-45-0Relevant articles and documents
3-Aryl-4-hydroxyquinolin-2(1H)-one derivatives as type I fatty acid synthase inhibitors
Rivkin, Alexey,Kim, Yoona R.,Goulet, Mark T.,Bays, Nathan,Hill, Armetta D.,Kariv, Ilona,Krauss, Stefan,Ginanni, Nicole,Strack, Peter R.,Kohl, Nancy E.,Chung, Christine C.,Varnerin, Jeffrey P.,Goudreau, Paul N.,Chang, Amy,Tota, Michael R.,Munoz, Benito
, p. 4620 - 4623 (2007/10/03)
A series of 3-aryl-4-hydroxyquinolin-2(1H)-ones with fatty acid synthase inhibitory activity was prepared. Starting from a derivative with an IC50 = 1.4 μM, SAR studies led to compounds with more than 70-fold increase in potency (IC50/sub
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 (2007/10/03)
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.