Synthesis and Anti-bvdv Activity of Acridones As New Potential Antiviral Agents.
From: Dipartimento di Chimica e Tecnologia del Farmaco, Università degli Studi di Perugia, Via del Liceo 1, 06123 Perugia, Italy. oriana.t@unipg.it
Journal of medicinal chemistry
- Publish Date: Apr 2006
- ISSN: 0022-2623
- Volume: 49
- Issue: 8
- Pages: 2621-7
- Medium: Print
- Language: English
- Citation (JAMA): Tabarrini Oriana, Manfroni Giuseppe, Fravolini Arnaldo, et al. Synthesis and Anti-bvdv Activity of Acridones As New Potential Antiviral Agents.. J. Med. Chem. Apr 2006;49:2621-7
Abstract
In this study we report the design, synthesis, and activity against bovine viral diarrhea virus (BVDV) of a novel series of acridone derivatives. BVDV is responsible for major losses in cattle. The virus is also considered to be a valuable surrogate for the hepatitis C virus (HCV) in antiviral drug studies. Some of the synthesized acridones elicited selective anti-BVDV activity with EC(50) values ranging from 0.4 to 4 microg/mL and were not cytotoxic at concentrations that were 25- to 200-fold higher (CC(50) >100 microg/mL). It was proven that the most potent acridone derivative 10 was able to not only protect cells from virus-induced cytopathic effect but also reduce the production of infectious virus and extracellular viral RNA. Furthermore, compound 10, as well as a number of other analogues, inhibited HCV replication to some extent. However, there was no direct correlation between anti-BVDV and anti-HCV activity. Thus, the acridone scaffold, when appropriately functionalized, can yield compounds with selective activity against pestiviruses and related viruses such as the HCV.
Mesh Headings (Keywords): Acridines, Animals, Antiviral Agents, Binding Sites, Cattle, Cell Proliferation, Diarrhea Viruses, Bovine Viral, Drug Design, Kidney, Microbial Sensitivity Tests, Molecular Structure, Structure-Activity Relationship, Virus Replication
Check for Full Text / PubMed Unique Identifier (PMID): 16610805
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