2-(2-Thienyl)-5, 6-dihydroxy-4-carboxypyrimidines as inhibitors of the hepatitis C virus NS5B polymerase: discovery, SAR, modeling, and mutagenesis

…, B Attenni, S Malancona, S Colarusso…

文献索引：Koch, Uwe; Attenni, Barbara; Malancona, Savina; Colarusso, Stefania; Conte, Immacolata; Di Filippo, Marcello; Harper, Steven; Pacini, Barbara; Giomini, Claudia; Thomas, Steven; Incitti, Ilario; Tomei, Licia; De Francesco, Raffaele; Altamura, Sergio; Matassa, Victor G.; Narjes, Frank Journal of Medicinal Chemistry, 2006 , vol. 49, # 5 p. 1693 - 1705

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被引用次数: 100

摘要

Infections caused by hepatitis C virus (HCV) are a significant world health problem for which novel therapies are in urgent demand. The polymerase of HCV is responsible for the replication of viral RNA. We recently disclosed dihydroxypyrimidine carboxylates 2 as novel, reversible inhibitors of the HCV NS5B polymerase. This series was further developed into 5, 6-dihydroxy-2-(2-thienyl) pyrimidine-4-carboxylic acids such as 34 (EC50 9.3 μM), which ...