221200-31-3

Upstream product

• 60456-26-0 (R)-glycidyl butyrate 
• 93246-54-9 3-fluoro-4-(pyrrolidin-1-yl)aniline 
• 369-34-6 3,4-difluoronitrobenzene 
• 221199-51-5 C₁₈H₁₉FN₂O₂ 

Downstream Products

• 221202-56-8 (S)-N'-benzoyl-N-[[3-[3-fluoro-4-(1-pyrrolidinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl]thiourea 
• 221200-93-7 (R)-5-Azidomethyl-3-(3-fluoro-4-pyrrolidin-1-yl-phenyl)-oxazolidin-2-one 
• 221201-27-0 (5S)-5-(aminomethyl)-3-(3-fluoro-4-pyrrolidin-1-ylphenyl)-1,3-oxazolidin-2-one 
• 221200-70-0 Methanesulfonic acid (R)-3-(3-fluoro-4-pyrrolidin-1-yl-phenyl)-2-oxo-oxazolidin-5-ylmethyl ester 

Relevant academic research and scientific papers

A method for the prevention or treatment of mycobacterial diseases

Disclosed in the present invention is a drug for preventing or treating mycobacterial diseases. In particular, disclosed is the use of a compound represented by the following general formula (I) or pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs thereof in preparing drugs for preventing or treating mycobacterial diseases, providing a new way for the prevention and treatment of tuberculosis and the like.

Design and synthesis of novel 5-acetylthiomethyl oxazolidinone analogs

The oxazolidinone class of antimicrobial agents represents a promising advance in the fight against resistant Gram-positive bacterial infections. To improve antibacterial activity and expand the spectrum of activity including Gram-negative bacteria, a series of novel 5-acetylthiomethyl oxazolidinone analogs were designed and synthesized based on the structure-activity relationship studies. The structures of the target compounds and main intermediates were confirmed by 1H NMR, 13C NMR, infrared (IR), mass spectra (MS), and elemental analysis.

Structure-activity relationship (SAR) studies on oxazolidinone antibacterial agents. 2.1) Relationship between lipophilicity and antibacterial activity in 5-thiocarbonyl oxazolidinones

5-Thiourea and 5-dithiocarbamate oxazolidinones were synthesized as a continuation of research on 5-thiocarbonyl oxazolidinone antibacterial agents considering the hydrophobic parameters of the molecule. The structure-activity relationship (SAR) study revealed that the antibacterial activity on 5-thiocarbonyl oxazolidinones was significantly affected by the lipophilicity, especially the calculated log P value and the balance between 5-hydrophilic (or hydrophobic) substituent and hydrophobic (or hydrophilic) substituents on the benzene ring. Some of 5-thiocarbonyl oxazolidinones were found to have good in vitro antibacterial activity against gram-positive bacteria including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE).