Merck
CN

Acridine derivatives as anti-BVDV agents.

Antiviral research (2011-05-31)
Michele Tonelli, Gerolamo Vettoretti, Bruno Tasso, Federica Novelli, Vito Boido, Fabio Sparatore, Bernardetta Busonera, Aicha Ouhtit, Pamela Farci, Sylvain Blois, Gabriele Giliberti, Paolo La Colla
ABSTRACT

Twenty-six 9-aminoacridine derivatives were evaluated in cell-based assays for cytotoxicity and antiviral activity against a panel of 10 RNA and DNA viruses. While seven compounds (9, 10, 14, 19, 21, 22, 24) did not affect any virus and two (6, 11) were moderately active against CVB-5 or Reo-1, 17 compounds exhibited a marked specific activity against BVDV, prototype of pestiviruses which are responsible for severe diseases of livestock. Most anti-BVDV agents showed EC(50) values in the range 0.1-8 μM, thus comparing favorably with the reference drugs ribavirine and NM 108. Some compounds, particularly those bearing a quinolizidinylalkyl side chain, displayed pronounced cytotoxicity. Further studies are warranted in order to achieve still better anti-BVDV agents, and to explore the potential antiproliferative activity of this kind of compounds.