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Molecules 2009, 14(12), 5189-5202; doi:10.3390/molecules14125189
Article

Synthesis and Evaluation of in Vitro Biological Activity of 4-Substituted Arylpiperazine Derivatives of 1,7,8,9-Tetrachloro-10,10-dimethoxy-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione

1, 1, 1,* , 2, 2, 3,* , 3, 3, 3 and 3
1 Department of Medical Chemistry, Medical University, 3 Oczki Str., 02-007 Warsaw, Poland 2 Faculty of Chemistry, Maria Curie-Sklodowska University, 20-031 Lublin, Poland 3 Department of Biomedical Science and Technology, University of Cagliari, Cittadella Universitaria, 09042, Monserrato, Cagliari, Italy
* Authors to whom correspondence should be addressed.
Received: 5 November 2009 / Revised: 26 November 2009 / Accepted: 1 December 2009 / Published: 11 December 2009
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Abstract

A series of twenty arylpiperazine derivatives of 1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo[5.2.1.02,6]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.
Keywords: 1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione; arylpiperazine derivatives; X-ray crystal structure analysis; antiviral activity 1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione; arylpiperazine derivatives; X-ray crystal structure analysis; antiviral activity
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Kossakowski, J.; Pakosinska-Parys, M.; Struga, M.; Dybala, I.; Koziol, A.E.; La Colla, P.; Marongiu, L.E.; Ibba, C.; Collu, D.; Loddo, R. Synthesis and Evaluation of in Vitro Biological Activity of 4-Substituted Arylpiperazine Derivatives of 1,7,8,9-Tetrachloro-10,10-dimethoxy-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione. Molecules 2009, 14, 5189-5202.

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