title: Antimicrobial and cytotoxic arylazoenamines. Part III: antiviral activity of selected classes of arylazoenamines.
abstract: Eighty-five arylazoenamines, characterized by different types of aryl and basic moieties, have been synthesized and evaluated in cell-based assays for cytotoxicity and antiviral activity against a panel of ten RNA and DNA viruses. The most commonly affected viruses were, in decreasing order, CVB-2, RSV, BVDV, YFV, and Sb-1; the remaining viruses were either not affected (HIV-1, VSV, and VV) or susceptible only to a very few compounds (Reo-1 and HSV-1). Thirty-five compounds exhibited high activity, with EC(50) in the range 0.8-10 microM, and other 28 compounds had EC(50) between 11 and 30 microM, thus indicating that the arylazoenamine molecular pattern is an interesting novel pharmacophore for antiviral agents against ssRNA viruses. Moreover, some compounds (as 28, 32, 42, and 53) appear of high interest, being devoid of toxicity on the human MT-4 cells (CC(50)>100 microM). A ligand-based computational approach was employed to identify highly predictive pharmacophore models for the most frequently affected viruses CVB-2, RSV, and BVDV. These models should allow the design of second generation of more potent inhibitors of these human and veterinary pathogens.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Genova, Viale Benedetto XV 3, 16132 Genova, Italy.
authors.forename: Michele
authors.initials: M
authors.lastname: Tonelli
authors.forename: Vito
authors.initials: V
authors.lastname: Boido
authors.forename: Caterina
authors.initials: C
authors.lastname: Canu
authors.forename: Anna
authors.initials: A
authors.lastname: Sparatore
authors.forename: Fabio
authors.initials: F
authors.lastname: Sparatore
authors.forename: Maria Silvia
authors.initials: MS
authors.lastname: Paneni
authors.forename: Maurizio
authors.initials: M
authors.lastname: Fermeglia
authors.forename: Sabrina
authors.initials: S
authors.lastname: Pricl
authors.forename: Paolo
authors.initials: P
authors.lastname: La Colla
authors.forename: Laura
authors.initials: L
authors.lastname: Casula
authors.forename: Cristina
authors.initials: C
authors.lastname: Ibba
authors.forename: David
authors.initials: D
authors.lastname: Collu
authors.forename: Roberta
authors.initials: R
authors.lastname: Loddo