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

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

【 摘 要 】

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.

【 授权许可】

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