Synthesis and anti-hepatitis C virus activity of novel ethyl 1H-indole-3-carboxylates in vitro.
A series of ethyl 1H-indole-3-carboxylates 9a(1)(-)(6) and 9b(1)(-)(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 9a(2) (>10; >16.7) and 9b(1) (>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 9a(3) (>6.25) was higher than that of ARB (6). Of these three initial hits, compound 9a(2) was the most potent.
Sellitto
Grazia
G
Dipartimento di Scienze Farmaceutiche,Università di Salerno, Fisciano, Italy. gsellitto@unisa.it
Faruolo
Aurora
A
de Caprariis
Paolo
P
Altamura
Sergio
S
Paonessa
Giacomo
G
Ciliberto
Gennaro
G
D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002264:Carboxylic Acids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D002460:Cell Line; D016174:Hepacivirus / Q000187:drug effects*; D006526:Hepatitis C / Q000188:drug therapy; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013440:Sulfides
D000998:Antiviral Agents; D002264:Carboxylic Acids; D007211:Indoles; C086979:umifenovir; D013440:Sulfides