Novel cycloalkylthiophene-imine derivatives bearing benzothiazole scaffold: synthesis, characterization and antiviral activity evaluation.
A series of novel cycloalkylthiophene-imine derivatives containing benzothiazole unit were designed, synthesized and evaluated for their anti-viral activities. The bio-evaluation results indicated that some of the target compounds (such as 5g, 5i, 5u) exhibited good to moderate antiviral effect on CVB5, ADV7 and EV71 viruses, however, these compounds did not have inhibition activity against H1N1 virus. Especially, the compounds 4c and 4d also exhibited high antiviral activities, which provide a new and efficient approach to evolve novel multi-functional antiviral agents by rational integration of active pharmacophores.
National Biopesticide Engineering Research Center, Hubei Academy of Agricultural Sciences, Wuhan 430064, People's Republic of China. keshaoyong@163.com
Shaoyong
S
Ke
Yanhong
Y
Wei
Ziwen
Z
Yang
Kaimei
K
Wang
Ying
Y
Liang
Liqiao
L
Shi
D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D052160:Benzothiazoles / Q000737:chemistry*; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D006367:HeLa Cells; D006801:Humans; D007097:Imines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D014780:Viruses / Q000187:drug effects* / Q000254:growth & development
D000998:Antiviral Agents; D052160:Benzothiazoles; D007097:Imines; D013876:Thiophenes; C005465:benzothiazole
Antiviral activity; Benzothiazole; Cycloalkylthiophene–imine; Synthesis