86872-96-0

Usage

InChI:InChI=1/C15H15NO/c1-2-16(14-6-4-3-5-7-14)15-10-8-13(12-17)9-11-15/h3-12H,2H2,1H3

Upstream product

• 1122-91-4 4-bromo-benzaldehyde 
• 103-69-5 N-ethyl-N-phenylamine 
• 606-99-5 N,N-diphenylethylamine 

Downstream Products

• 95548-99-5 (E)-2,3-Bis-[4-(ethyl-phenyl-amino)-phenyl]-but-2-enedinitrile 
• 95549-04-5 2,3-Bis-[4-(ethyl-phenyl-amino)-phenyl]-succinonitrile 
• 190599-55-4 4-(N-ethyl-N-phenylamino)styrene 

Relevant academic research and scientific papers

Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant

On the basis of our earlier discovery of N1-selective inhibitors, the 150-cavity of influenza virus neuraminidases (NAs) could be further exploited to yield more potent oseltamivir derivatives. Among the synthesized compounds, 15b and 15c were exceptionally active against both group-1 and -2 NAs. Especially for 09N1, N2, N6, and N9 subtypes, they showed 6.80-12.47 and 1.20-3.94 times greater activity than oseltamivir carboxylate (OSC). They also showed greater inhibitory activity than OSC toward H274Y and E119V variant. In cellular assays, they exhibited greater potency than OSC toward H5N1, H5N2, H5N6, and H5N8 viruses. 15b demonstrated high metabolic stability, low cytotoxicity in vitro, and low acute toxicity in mice. Computational modeling and molecular dynamics studies provided insights into the role of R group of 15b in improving potency toward group-1 and -2 NAs. We believe the successful exploitation of the 150-cavity of NAs represents an important breakthrough in the development of more potent anti-influenza agents.

A oseltamivir derivative and its preparation method and application (by machine translation)

The invention discloses a oseltamivir derivative and its preparation method and application. The derivatives of general formula I has the structure shown, the invention also discloses a method for the preparation of oseltamivir derivatives, can be for influenza virus neuraminidase inhibitors, and containing one or more of composition in the preparation of anti-influenza virus drugs in the application. (by machine translation)