Synthesis and in vitro-Anti-hepatitis B Virus Activities of Several Ethyl 5-Hydroxy-1H-indole-3-carboxylates1
Chun-shen ZHAOa, Yan-fang ZHAOa, Hui-fang CHAIa and Ping GONGCorresponding Author Contact Information, a, E-mail The Corresponding Author
aLiaoning Province Key Laboratory of Innovative Medicine Research and Design, Shenyang Pharmaceutical University, Shenyang 110016, P. R. China
Received 10 October 2005.
Available online 11 October 2006.
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.
Volume 22, Issue 5, September 2006, Pages 577-583
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http://dx.doi.org/10.1016/S1005-9040(06)60166-9 