126202-89-9

Basic information

• Product Name: Dalfopristin+Quinupristin
• Synonyms: Dalfopristin+Quinupristin
• CAS NO: 126202-89-9
• Molecular Formula: C₁₈H₁₂ClN₃
• Molecular Weight: 305.76098
• Mol File: 126202-89-9.mol
• Article Data: 1

Chemical Properties

• Melting Point: 226 °C
• Boiling Point: 527.3±50.0 °C(Predicted)
• Appearance: /
• Density: 1.34±0.1 g/cm3(Predicted)
• PKA: 2.40±0.18(Predicted)
• CAS DataBase Reference: Dalfopristin+Quinupristin(CAS DataBase Reference)
• NIST Chemistry Reference: Dalfopristin+Quinupristin(126202-89-9)
• EPA Substance Registry System: Dalfopristin+Quinupristin(126202-89-9)

Safety Data

• Hazardous Substances Data: 126202-89-9(Hazardous Substances Data)

Usage

Clinical Use

A drug combination of the streptogramins, quinupristin and dalfopristin was approved for IV use in the treatment of infections caused by vancomycin-resistant Enterococcus faeci um bacteremia as well as skin/skin structure infections caused by MRSA and methicillin-sensitive Streptococcus pyogenes. Certain strains of E. faecium are resistant to essentially all other antibiotics, including vancomycin. The streptogramin type A compound dalfopristin binds to the 50S ribosomal subparticle, resulting in a conformational change in the substrate. It appears that dalfopristin binding creates a high-affinity binding site for quinupristin, accounting for the synergy.

Upstream product

• 587-04-2 m-Chlorobenzaldehyde 
• 98-86-2 acetophenone 
• 109-77-3 malononitrile 

Relevant articles and documents

Discovery of colon tumor cell growth inhibitory agents through a combinatorial approach

Two series with the general formula of 4,6-diaryl-2-oxo-1,2 dihydropyridine-3-carbonitriles and their isosteric 4,6-diaryl-2-imino-1,2-dihydropyridine-3-carbonitrile were synthesized through one pot reaction of the appropriate acetophenone, aldehyde, ammonium acetate with ethyl cyanoacetate or malononitrile, respectively. The synthesized compounds were evaluated for their tumor cell growth inhibitory activity against the human HT-29 colon tumor cell line, as well as their PDE3 inhibitory activity. Compound 4-(2-Ethoxyphenyl)-2-oxo-6-thiophen-3-yl-1,2-dihydropyridine-3 carbonitrile (21) showed tumor cell growth inhibitory activity with an IC50 value of 1.25 μM. Meanwhile, 4-(4-Ethoxyphenyl)-2-imino-6-(thiophen-3-yl)-1,2-dihydropyridine-3-carbonitrile (26) showed inhibitory effect upon PDE3 using cAMP or cGMP as substrate. No correlation exists between PDE3 inhibition and the tumor cell growth inhibitory activity. Docking compound 21 to other possible molecular targets showed the potential to bind PIM1 Kinase.