952150-41-3

Upstream product

• 1138150-46-5 [1,2,5]triazepane-1-carboxylic acid tert-butyl ester 
• 952150-39-9 5(R)-(hydroxymethyl)-3-(3,5-difluoro-4-(1-(benzyloxycarbonyl)-2-(tert-butoxycarbonyl)[1,2,5]triazepan-5-yl)phenyl)oxazolidin-2-one 
• 952150-38-8 5-(4-benzyloxycarbonylamino-2,6-difluorophenyl)[1,2,5]triazepane-1,2-dicarboxylic acid 1-benzyl ester 2-tert-butyl ester 
• 1443005-31-9 5-(2,6-difluoro-4-nitrophenyl)[1,2,5]triazepane-1-carboxylic acid tert-butyl ester 
• 66684-58-0 3,4,5-trifluoronitrobenzene 
• 952150-40-2 5(R)-(azidomethyl)-3-(3,5-difluoro-4-(1-(benzyloxycarbonyl)-2-(tert-butoxycarbonyl)[1,2,5]triazepan-5-yl)phenyl)oxazolidin-2-one 

Downstream Products

• 952150-42-4 5(S)-(acetylaminomethyl)-3-(3,5-difluoro-4-(1-(tertbutoxycarbonyl)[1,2,5]triazepan-5-yl)phenyl)oxazolidin-2-one 
• 952151-26-7 (S)-N-((3-(3,5-difluoro-4-(1-(hydroxyacetyl)[1,2,5]triazepan-5-yl)phenyl)-2-oxo-5-oxazolidinyl)methyl)acetamide 

Relevant academic research and scientific papers

Antibacterial oxazolidinone analogues having a N-hydroxyacetyl-substituted seven-membered [1,2,5]triazepane or [1,2,5]oxadiazepane C-ring unit

We synthesized a series of oxazolidinone analogues bearing a N-hydroxyacetyl-substituted [1,2,5]triazepane or [1,2,5]oxadiazepane C-ring unit as homologues of an earlier drug candidate, eperezolid. Several of these compounds exhibited potent in vitro antibacterial activities towards not only Gram-positive, but also Gram-negative and linezolid-resistant pathogens. Compounds 21a and 21b, bearing a thiocarbamate side chain, showed high in vivo activity against methicillin-resistant Staphylococcus aureus SR3637, together with a promising safety profile in terms of weak inhibition of monoamine oxidase and cytochrome P450 isozymes.

NOVEL COMPOUND HAVING HETEROCYCLIC RING

The invention provides a novel oxazolidinone derivative represented by the formula (I): wherein Ring A is optionally substituted or fused and represents (A-1) at least 7-membered monocyclic hetero ring containing at least three N atoms; (A-2) at least 6-membered monocyclic hetero ring containing at least two N atoms and at least one O atom; or (A-3) at least 7-membered monocyclic hetero ring containing at least two N atoms and at least one S atom; X1 is a single bond, -O-, -S-, -NR2-, -CO-, -CS-, - CONR3-, -NR4CO-, -SO2NR5-, and -NR6SO2- (wherein R2 - R6 are independently hydrogen or lower alkyl), or lower alkylene or lower alkenylene in which one of the preceding groups may intervene; Ring B is optionally substituted carbocycle or optionally substituted heterocycle; R1 is hydrogen, or an organic residue which is able to bind to the 5-position of oxazolidinone ring in oxazolidinone antimicrobial agent, and an antibacterial agent containing the same.