Synthesis and evaluation of in vitro biological activity of 4-substituted arylpiperazine derivatives of 1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo[5.2.1.0(2,6)]dec-8-ene-3,5-dione

A series of twenty arylpiperazine derivatives of 1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo[5.2.1.0(2,6)]dec-8-ene-3,5-dione have been prepared. These derivatives were tested in vitro with the aim of identifying novel lead compounds active against emergent and re-emergent human and cattle inf...

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Published in:Molecules (Basel, Switzerland) Switzerland), 2009-12, Vol.14 (12), p.5189-5202
Main Authors: Kossakowski, Jerzy, Pakosinska-Parys, Magdalena, Struga, Marta, Dybala, Izabela, Koziol, Anna E, La Colla, Paolo, Marongiu, Laura Ester, Ibba, Cristina, Collu, David, Loddo, Roberta
Format: Article
Language:English
Subjects:
1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione
Animals
antiviral activity
Antiviral Agents - chemical synthesis
Antiviral Agents - pharmacology
arylpiperazine derivatives
Biological activity
Cell Line
Crystallography, X-Ray
Dengue fever
Diarrhea
Drug Evaluation, Preclinical
Encephalitis
Hepatitis C
Heterocyclic Compounds, 3-Ring - chemical synthesis
Heterocyclic Compounds, 3-Ring - pharmacology
In Vitro Techniques
Infections
Infectious diseases
Microbial Sensitivity Tests
Models, Molecular
Molecular Structure
Tropical diseases
Viruses
West Nile virus
X-ray crystal structure analysis
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Summary:A series of twenty arylpiperazine derivatives of 1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo[5.2.1.0(2,6)]dec-8-ene-3,5-dione have been prepared. These derivatives were tested in vitro with the aim of identifying novel lead compounds active against emergent and re-emergent human and cattle infectious diseases (AIDS, hepatitis B and C, tuberculosis, bovine viral diarrhea). In particular, these compounds were evaluated in vitro against representatives of different virus classes, such as a HIV-1 (Retrovirus), a HBV (Hepadnavirus) and the single-stranded RNA(+) viruses Yellow fever virus (YFV) and Bovine viral diarrhea virus (BVDV), both belonging to the Flaviridae. Compounds 2c, 2g and 3d showed a modest activity against CVB-2. The molecular structures of the starting imide 1 and one of propyl-piperazine derivatives, 3b, have been determined by an X-ray crystallography study.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules14125189