Unsymmetrical methylene derivatives 5 were prepared following a well experienced way, by reacting the Mannich bases of 2-naphthols 4 with indoles. All synthesized compounds were tested against a wide panel of viruses, since previous works showed that Mannich bases on 7-hydroxycoumarin 1 and unsymmetrical methylene derivatives 2 were endowed with an interesting antiviral activity. Now, the symmetrical Mannich bases 4 were completely inactive, whereas the unsymmetrical methylene derivatives 5, although possessing a certain degree of toxicity, showed a remarkable activity against RSV. Some of compounds 5 showed a moderate antiviral activity also 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.
Antiviral Activity of Indole Derivatives
BALBI, ALESSANDRO;MAZZEI, MAURO;
2009-01-01
Abstract
Unsymmetrical methylene derivatives 5 were prepared following a well experienced way, by reacting the Mannich bases of 2-naphthols 4 with indoles. All synthesized compounds were tested against a wide panel of viruses, since previous works showed that Mannich bases on 7-hydroxycoumarin 1 and unsymmetrical methylene derivatives 2 were endowed with an interesting antiviral activity. Now, the symmetrical Mannich bases 4 were completely inactive, whereas the unsymmetrical methylene derivatives 5, although possessing a certain degree of toxicity, showed a remarkable activity against RSV. Some of compounds 5 showed a moderate antiviral activity also 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.
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