1443005-68-2

Upstream product

• 952151-39-2 [1,2,5]oxadiazepane-2-carboxylic acid tert-butyl ester 
• 264600-97-7 3-N-(t-butoxycarbonyl)amino-1,2-isoxazole 
• 952151-43-8 5(R)-(hydroxymethyl)-3-(3,5-difluoro-4-(2-(tertbutoxycarbonyl)[1,2,5]oxadiazepan-5-yl)phenyl)oxazolidin-2-one 
• 952151-42-7 5-(4-benzyloxycarbonylamino-2,6-difluorophenyl)[1,2,5]oxadiazepane-2-carboxylic acid tert-butyl ester 
• 952151-41-6 5-(2,6-difluoro-4-nitrophenyl)[1,2,5]oxadiazepane-2-carboxylic acid tert-butyl ester 
• 66684-58-0 3,4,5-trifluoronitrobenzene 

Downstream Products

• 1138150-19-2 5(S)-(isoxazol-3-yl-aminomethyl)-3-(3,5-difluoro-4-(2-(hydroxyacetyl)[1,2,5]oxadiazepan-5-yl)phenyl)oxazolidin-2-one 
• 1443005-71-7 5(S)-(isoxazol-3-yl-aminomethyl)-3-(3,5-difluoro-4-([1,2,5]oxadiazepan-5-yl)phenyl)oxazolidin-2-one 

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.