Synthesis and anti-hepatitis C virus activity of novel ethyl 1H-indole-3-carboxylates in vitro

Add time:09/07/2019    Source:sciencedirect.com

A series of ethyl 1H-indole-3-carboxylates 9a1–6 and 9b1–2 were prepared and evaluated in Huh-7.5 cells. Most of the compounds exhibited anti-hepatitis C virus (HCV) activities at low concentration. The selectivity indices of inhibition on entry and replication of compounds 9a2 (>10; >16.7) and 9b1 (>6.25; >16.7) were higher than those of the other evaluated compounds, including the lead compound Arbidol (ARB, 6; 15). Moreover, the selective index of inhibition on entry of compound 9a3 (>6.25) was higher than that of ARB (6). Of these three initial hits, compound 9a2 was the most potent.

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