232950-90-2

Upstream product

• 100-97-0 hexamethylenetetramine 
• 139071-79-7 (S)-N-[[3-(3-fluorophenyl)-2-oxo-5-oxazolidinyl]methyl]acetamide 
• 1428246-76-7 5-(S)-acetamidomethyl-3-[4'-dimethoxymethyl-3'-fluorophenyl]-oxazolidine-2-one 
• 1427-07-2 2-fluoro-4-nitrotoluene 
• 840501-17-9 [4-(tert-butyl-dimethyl-silanyloxymethyl)-3-fluoro-phenyl]-carbamic acid benzyl ester 
• 840501-16-8 (3-fluoro-4-hydroxymethyl-phenyl)-carbamic acid benzyl ester 
• 840501-15-7 (4-amino-2-fluorophenyl)methanol 
• 73792-08-2 methyl 4-amino-2-fluorobenzoate 
• 392-09-6 2-fluoro-4-nitro-benzoic acid methyl ester 
• 403-24-7 2-fluoro-4-nitrobenzoic acid 

Relevant academic research and scientific papers

The synthesis and antimicrobial evaluation of a new series of isoxazolinyl oxazolidinones

A series of oxazolidinone antibacterial agents containing a 5-substituted isoxazol-3-yl moiety were synthesized via a nitrile oxide [3+2] dipolar cycloaddition reaction. These compounds were screened against a panel of susceptible and resistant Gram-positive organisms. Several analogs from this series were comparable to or more potent than linezolid in vitro.

Effects of positional and geometrical isomerism on the biological activity of some novel oxazolidinones

Some novel oxazolidinone derivatives have been synthesized and tested for antibacterial activity. Compound 13 was found to be active against Gram-positive pathogens whereas compound 14 was less active. Either less active or inactive molecules were obtained, when benzotriazole was replaced with benzimidazole, benzthiazole, or benzoxazole. However, thioacetamide analogue of 13 produced a potent molecule similar to linezolid in vitro. Some novel oxazolidinone derivatives with benzotriazole as pendant have been synthesized and tested for antibacterial activity. Linearly attached benzotriazole derivative showed more potency compared to angular one in vitro. Out of E/Z-isomers of angularly attached derivatives E-isomer was found to be more potent than Z-isomer. Either less active or inactive molecules were obtained, when benzotriazole was replaced with benzimidazole, benzthiazole, or benzoxazole. Finally, thioacetamide analogue of linear compound gave a lead having activity similar to linezolid in vitro.

Oxazolidinone combinatorial libraries, compositions and methods of preparation

Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.