ORIGINAL ARTICLE
Synthesis and antiviral activity of some novel indole-2-carboxylate derivatives

https://doi.org/10.1016/j.apsb.2014.06.003Get rights and content
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Abstract

A series of novel indole-2-carboxylate derivatives were synthesized and assayed to determine their in vitro broad-spectrum antiviral activities. The biological results showed that some of the synthesized compounds exhibited potent broad-spectrum antiviral activity. Notably, compound 8f showed the highest SI value (17.1) to Cox B3 virus. Compound 14f showed both potent inhibitory activity against influenza A (IC50=7.53 μmol/L) and the highest SI value (12.1). SAR results showed that the alkyloxy at the 4-position of indole ring was not crucial to the antiviral activities. Incorporation of an acetyl substituent at the amino group disfavored antiviral activity towards RNA viruses.

Graphical abstract

Compound 8f showed the highest SI value (17.1) to Cox B3 virus. Compound 14f showed both potent inhibitory activity against influenza A (IC50=7.53 μmol/L) and the highest SI value (12.1).

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KEY WORDS

Indole-2-carboxylate
Broad-spectrum antiviral activity
DNA and RNA virus
SAR

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Peer review under responsibility of Institute of Materia Medica, Chinese Academy of Medical Sciences and Chinese Pharmaceutical Association.

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