piperidines has been researched along with chlorobenzene* in 1 studies
1 other study(ies) available for piperidines and chlorobenzene
| Article | Year |
|---|---|
Discovery and evolution of aloperine derivatives as novel anti-filovirus agents through targeting entry stage.
Preventing filoviruses in the entry stage is an attractive antiviral strategy. Taking aloperine, a Chinese natural herb with an endocyclic skeleton, as the lead, 23 new aloperine derivatives were synthesized and evaluated for their anti-filovirus activities including ebola virus (EBOV) and marburg virus (MARV) using pseudotyped virus model. Structure-activity relationship (SAR) analysis indicated that the introduction of a 12N-dichlorobenzyl group was beneficial for the potency. Compound 2e exhibited the most potent anti-EBOV and anti-MARV effects both in vitro and in vivo. It also displayed a good pharmacokinetic and safety profile in vivo, indicating an ideal druglike feature. The primary mechanism study showed that 2e could block a late stage of viral entry, mainly through inhibiting cysteine cathepsin B activity of host components. We consider compound 2e to be a promising broad-spectrum anti-filovirus agent with the advantages of a unique chemical scaffold and a specific biological mechanism. Topics: Antiviral Agents; Cathepsin B; Chlorobenzenes; Filoviridae; Humans; Piperidines; Quinolizidines; Structure-Activity Relationship; Virus Internalization | 2018 |