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

被引:16
|
作者
Kossakowski, Jerzy [1 ]
Pakosinska-Parys, Magdalena [1 ]
Struga, Marta [1 ]
Dybala, Izabela [2 ]
Koziol, Anna E.
La Colla, Paolo [2 ,3 ]
Marongiu, Laura Ester [3 ]
Ibba, Cristina [3 ]
Collu, David [3 ]
Loddo, Roberta [3 ]
机构
[1] Med Univ, Dept Med Chem, PL-02007 Warsaw, Poland
[2] Marie Curie Sklodowska Univ, Fac Chem, PL-20031 Lublin, Poland
[3] Univ Cagliari, Dept Biomed Sci & Technol, I-09042 Cagliari, Italy
关键词
1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo[5.2.1.0(2,6)]dec-8-ene-3,5-dione; arylpiperazine derivatives; X-ray crystal structure analysis; antiviral activity; INHIBITORS; HEPATITIS; PATHOGENESIS; REPLICATION;
D O I
10.3390/molecules14125189
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
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.
引用
收藏
页码:5189 / 5202
页数:14
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