Antiviral activity of indole derivatives.
Unsymmetrical methylene derivatives 5 were prepared following a known method, by reaction of the Mannich bases of 2-naphthols 4 with indoles. All synthesized compounds were tested against a wide panel of viruses, since previous work showed that Mannich bases on 7-hydroxycoumarin 1 and unsymmetrical methylene derivatives 2 were endowed with some antiviral activities. The symmetrical Mannich bases 4 were completely inactive, whereas the unsymmetrical methylene derivatives 5, although possessing a certain degree of toxicity, showed a significant activity against RSV. Some of compounds 5 showed a moderate antiviral activity against HIV-1, BVDV, YFV and CVB-2. The lack of activity of Mannich bases 4 demonstrates the crucial importance for antiviral activity of coumarin moiety present in Mannich bases 1.
Giampieri
Michele
M
Department of Pharmaceutical Sciences, University of Genoa, Genoa, Italy.
Balbi
Alessandro
A
Mazzei
Mauro
M
La Colla
Paolo
P
Ibba
Cristina
C
Loddo
Roberta
R
D000818:Animals; D000998:Antiviral Agents; D002460:Cell Line; D030241:Diarrhea Virus 1, Bovine Viral / Q000187:drug effects; D004770:Enterovirus / Q000187:drug effects; D015497:HIV-1 / Q000187:drug effects; D007211:Indoles / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D012136:Respiratory Syncytial Viruses / Q000187:drug effects; D015005:Yellow fever virus / Q000187:drug effects
D000998:Antiviral Agents; D007211:Indoles