Synthesis and in vitro-Anti-hepatitis B Virus Activities of Several Ethyl 5-Hydroxy-1H-indole-3-carboxylates1

A series of ethyl 5-hydroxyindole-3-carboxylates 6a-10r was designed and synthesized. The structures of all the compounds were confirmed by IR, 1H NMR, and MS and their anti-hepatitis B virus (HBV) activities were evaluated in 2. 2. 15 cells. Among them, compound 7g {ethyl 5-hydroxy-2-[(3-methoxyphenylsulfinyl) methyl]-1-methyl-4-[(4-methylpiperazin-1-yl)methyl]-1H-indole-3-carboxylate} displays a significant anti-HBV activity, which is more potent than the positive control lamivudine.