1341209-33-3

Upstream product

• 321-23-3 4-bromo-2-fluoronitrobenzene 
• 911845-41-5 benzyl (4-bromo-2-(((2R,3S)-3-(hydroxymethyl)oxiran-2-yl)methoxy)phenyl)carbamate 
• 911845-45-9 (3R,3aS)-7-bromo-3-((1,1-dimethylethyl)dimethylsilanemethyl)-3a,4-dihydro-3H-[1,3]oxazolo[4,3-c][1,4]benzoxazin-1-one 
• 911845-39-1 benzyl (Z)-(4-bromo-2-((4-hydroxybut-2-en-1-yl)oxy)phenyl)carbamate 
• 121-51-7 3-nitrobenzenesulphonyl chloride 
• 911845-37-9 (2Z)-4-(5-bromo-2-nitrophenoxy)but-2-en-1-ol 

Downstream Products

• 1341208-56-7 N-{[(3S,3aS)-7-(3-nitrophenyl)-1-oxo-1,3,3a,4-tetrahydrobenzo[b]oxazolo[3,4-d][1,4]oxazin-3-yl]methyl}acetamide 
• 1341208-57-8 N-{[(3S,3aS)-7-(4-cyanophenyl)-1-oxo-1,3,3a,4-tetrahydrobenzo[b]oxazolo[3,4-d][1,4]oxazin-3-yl]methyl}acetamide 
• 1341208-59-0 N-{[(3S,3aS)-7-(3-aminophenyl)-1-oxo-1,3,3a,4-tetrahydrobenzo[b]oxazolo[3,4-d][1,4]oxazin-3-yl]methyl}acetamide 
• 1341208-58-9 N-{[(3S,3aS)-7-(4-acetylphenyl)-1-oxo-1,3,3a,4-tetrahydrobenzo[b]oxazolo[3,4-d][1,4]oxazin-3-yl]methyl}acetamide 
• 1341208-55-6 N-{[(3S,3aS)-1-oxo-7-phenyl-1,3,3a,4-tetrahydrobenzo[b]oxazolo[3,4-d][1,4]oxazin-3-yl]methyl}acetamide 

Relevant academic research and scientific papers

Synthesis and biological evaluation of novel benzoxazinyl-oxazolidinones as potential antibacterial agents

A number of benzoxazinyl-oxazolidinones bearing 3-trizolylmethyl or 3-carboxamide side chain were designed and synthesized with the aim to develop antibacterial agents with improved properties. In vitro antibacterial activities of these novel compounds we

NOVEL BENZOXAZINE OXAZOLIDINONE COMPOUNDS, PREPARATION METHODS AND USES THEREOF

Novel benzoxazine oxazolidinone compounds, preparation methods and uses thereof are disclosed, which belong to the field of pharmacy. More specifically, novel benzoxazine oxazolidinone compounds represented by the following formula (I), preparation method

Design, synthesis, and structure-activity relationship studies of highly potent novel benzoxazinyl-oxazolidinone antibacterial agents

A series of novel benzoxazinyl-oxazolidinones bearing nonaromatic heterocycle or aryl groups were designed and synthesized. Their in vitro and in vivo antibacterial activities were investigated. Most of the (3S, 3aS) biaryl benzoxazinyl-oxazolidinones exhibited potent activity against Gram-positive pathogens. SAR trends were observed; a pyridyl C ring was preferable to other 5- or 6-member aryl C rings, while fluorine substitution on the B ring generated derivatives with reduced activity. Various substituent group positions on the pyridyl ring were also evaluated. The resulting compounds displayed excellent activity against linezolid-resistant strains. Compound 45 exhibited excellent in vitro activity, with a MIC value of 0.25-0.5 μg/mL against MRSA and an activity against linezolid-resistant strains of 8-16-fold higher potency than linezolid. In a MRSA systemic infection model, compound 45 displayed an ED 50 5.0 mg/kg, a potency that is nearly 3-fold better than that of linezolid. This compound also showed excellent pharmacokinetic profiles, with a half-life of more than 5 h as well as an oral bioavailability of 81% in rats.