40000-89-3

Usage

InChI:InChI=1/C9H8N2O/c1-6-5-7-3-2-4-10-8(7)11-9(6)12/h2-5H,1H3,(H,10,11,12)

Upstream product

• 127446-48-4 3-[2-(2,2-Dimethyl-propionylamino)-pyridin-3-yl]-3-hydroxy-2-methyl-propionic acid tert-butyl ester 
• 7521-41-7 2-Aminonicotinaldehyde 
• 79-03-8 propionyl chloride 
• 1126425-11-3 C₁₂H₁₄N₂O₃ 

Downstream Products

• 1126424-63-2 C₉H₆BrClN₂ 

Relevant academic research and scientific papers

Lead Optimization of Influenza Virus RNA Polymerase Inhibitors Targeting PA-PB1 Interaction

Influenza viruses are responsible for contagious respiratory illnesses in humans and cause seasonal epidemics and occasional pandemics worldwide. Previously, we identified a quinolinone derivative PA-49, which inhibited the influenza virus RNA-dependent RNA polymerase (RdRp) by targeting PA-PB1 interaction. This paper reports the structure optimization of PA-49, which resulted in the identification of 3-((dibenzylamino)methyl)quinolinone derivatives with more potent anti-influenza virus activity. During the optimization, the hit compound 89, which was more active than PA-49, was identified. Further optimization and scaffold hopping of 89 led to the most potent compounds 100 and a 1,8-naphthyridinone derivative 118, respectively. We conclusively determined that compounds 100 and 118 suppressed the replication of influenza virus and exhibited anti-influenza virus activity against both influenza virus types A and B in the range of 50% effective concentration (EC50) = 0.061-0.226 μM with low toxicity (50% cytotoxic concentration (CC50) >10 μM).

NOVEL PI3K p110 INHIBITORS AND METHODS OF USE THEREOF

The invention includes compositions that regulated PI3K p110 delta and are useful as an anti-viral therapy. The invention includes a method of inhibiting p110 delta, a component of PI3K p110 delta signaling pathway, or any combination thereof in a cell as

TETRACYCLIC INDOLE DERIVATIVES AND METHODS OF USE THEREOF

The present invention relates to Tetracyclic Indole Derivatives, compositions comprising at least one Tetracyclic Indole Derivative, and methods of using the Tetracyclic Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.

2,3-SUBSTITUTED AZAINDOLE DERIVATIVES FOR TREATING VIRAL INFECTIONS

The present invention relates to 2,3-Substituted Azaindole Derivatives, compositions comprising at least one 2,3-Substituted Azaindole Derivatives, and methods of using the 2,3-Substituted Azaindole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.

SUBSTITUTED INDOLE DERIVATIVES AND METHODS OF USE THEREOF

The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.

TRICYCLIC INDOLE DERIVATIVES AND METHODS OF USE THEREOF

The present invention relates to Tricyclic Indole Derivatives, compositions comprising at least one Tricyclic Indole Derivatives, and methods of using the Tricyclic Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient

New heteroaryl-spaced phosphono α-amino acids are competitive NMDA antagonists with analgesic activity

The synthesis and the NMDA receptor binding affinities of α-amino-3-(phosphonomethyl)-2-naphthalenepropanoic acid, α-amino-3-(phosphonomethyl)-2-benzofuranpropanoic acid, a series of substituted (R)-α-amino-3-(phosphonomethyl)-2-quinolinepropanoic acids, (R)-α-amino-3-(phosphonomethyl)-1,8-naphthyridine-2-propanoic acid and (R)-α-amino-3-(phosphonomethyl)-1,6-naphthyridine-2-propanoic acid are reported.

A General Approach to the Synthesis of 1,6-, 1,7-, and 1,8-Naphthyridines

A new three-step procedure for pyridine annulation is described and illustrated with efficient syntheses of various 1,6-, 1,7-, and 1,8-naphthyridin-2-ones as well as 6-chloroquinolin-2-one.The regiospecific ortho metalation and subsequent formylation of