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

Chemical Research in Chinese Universities ›› 2006, Vol. 22 ›› Issue (5): 577-583.doi:

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

ZHAO Chun-shen, ZHAO Yan-fang, CHAI Hui-fang and GONG Ping

Liaoning Province Key Laboratory of Innovative Medicine Research and Design, Shenyang Pharmaceutical University, Shenyang 110016, P. R. China

Received:2005-10-10 Revised:1900-01-01 Online:2006-09-25 Published:2006-09-25
Contact: GONG Ping E-mail:gongpinggp@126.com

Abstract

Abstract: 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.

Key words: Ethyl 5-hydroxy-1H-indole-3-carboxylates, Synthesis, Anti-hepatitis B virus activity

ZHAO Chun-shen, ZHAO Yan-fang, CHAI Hui-fang , GONG Ping. Synthesis and in vitro-Anti-hepatitis B Virus Activities of Several Ethyl 5-Hydroxy-1H-indole-3-carboxylates[J]. Chemical Research in Chinese Universities, 2006, 22(5): 577-583.

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

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