期刊论文详细信息
Molecules
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
Jerzy Kossakowski1  Magdalena Pakosinska-Parys1  Marta Struga1  Izabela Dybala1  Anna E. Koziol1  Paolo La Colla1  Laura Ester Marongiu1  Cristina Ibba1  David Collu1 
[1] 1Department of Medical Chemistry, Medical University, 3 Oczki Str., 02-007 Warsaw, Poland 2Faculty of Chemistry, Maria Curie-Sklodowska University, 20-031 Lublin, Poland 3Department of Biomedical Science and Technology, University of Cagliari, Cittadella Universitaria, 09042, Monserrato, Cagliari, Italy
关键词: 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;   
DOI  :  10.3390/molecules14125189
来源: mdpi
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【 摘 要 】

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.

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This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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