30384-79-3Relevant articles and documents
Anti-BVDV activity evaluation of naphthoimidazole derivatives compared with parental imidazoquinoline compounds
Carta, Antonio,Delogu, Ilenia,Ibba, Roberta,Loddo, Roberta,Piras, Sandra
, p. 65 - 70 (2020/10/06)
Background: Pestivirus genus includes animal pathogens which are involved in economic impact for the livestock industry. Among others, Bovine Viral Diarrhoea Virus (BVDV) establish a persistent infection in cattle causing a long list of symptoms and a high mortality rate. In the last decades, we synthesised and reported a certain number of anti-BVDV compounds. Methods: In them, imidazoquinoline derivatives turned out as the most active. Their mechanism of actions has been deeply investigated, BVDV RNA-dependent RNA polymerase (RpRd) resulted as target and the way of binding was predicted in silico through three main H-bond interaction with the target. The prediction could be confirmed by target or ligand mutation. The first approach has already been performed and published confirming the in silico prediction. Results: Here, we present how the ligand chemical modification affects the anti-BVDV activity. The designed compounds were synthesised and tested against BVDV as in silico assay negative control. Conclusion: The antiviral results confirmed the predicted mechanism of action, as the newly synthesised compounds resulted not active in the in vitro BVDV infection inhibition.
Synthesis of 2-arylbenzimidazole analogues
Chang, Meng-Yang,Chan, Chieh-Kai,Chen, Yi-Chia
, p. 1229 - 1236 (2014/05/20)
Substituted 2-arylbenzimidazoles (4) were easily synthesized in good yields starting from the condensation reaction of 1,2-diaminobenzenes (1) with β-ketosulfones (5) in the presence of boiling HOAc.
Copper-catalyzed synthesis of benzazoles via aerobic oxidative condensation of o-amino/mercaptan/hydroxyanilines with benzylamines
Xiao, Tiebo,Xiong, Shengwei,Xie, Yang,Dong, Xichang,Zhou, Lei
, p. 15592 - 15595 (2013/09/12)
A simple and efficient method for the synthesis of benzazoles via Cu-catalyzed aerobic oxidative condensation of o-amino/mercaptan/hydroxyanilines with benzylamines was developed.