Antiviral activity of indole derivatives

GIAMPIERI M;BALBI A;MAZZEI M;LA COLLA P;IBBA, CRISTINA;LODDO, ROBERTA

2009-01-01

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Abstract

Unsymmetrical methylene derivatives 5 were prepared following a known method, by reaction of the Mannich bases of 2-naphthols 4 with indoles. All synthesizedcompoundswere 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.