87508-45-0Relevant academic research and scientific papers
BIFUNCTIONAL HETEROCYCLIC COMPOUNDS AND METHODS OF MAKING AND USING SAME
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Page/Page column 264; 265, (2010/02/06)
The invention provides a family of bifunctional heterocyclic compounds useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. The invention also provides methods of making the bifunctional hetercyclic compounds, and methods of using such compounds as anti-infective, anti-proliferative agents, anti-inflammatory, and/or prokinetic agents.
Antibacterials. Synthesis and structure-activity studies of 3-aryl-2-oxooxazolidines. 1. The 'B' group
Gregory,Brittelli,Wang,Wuonola,McRipley,Eustice,Eberly,Bartholomew,Slee,Forbes
, p. 1673 - 1681 (2007/10/02)
The synthesis and structure/activity studies of the effect of varying the 'B' group in a series of oxazolidinone antibacterials (I) are described. Two synthetic routes were used: (1) alkylation of aniline with glycidol followed by dialkyl carbonate heterocyclization to afford I (A = H, B = OH), whose arene ring was further elaborated by using electrophilic aromatic substitution methodology; (2) cycloaddition of substituted aryl isocyanates with epoxides to give A and B with a variety of values. I with B = OH or Br were converted to other 'B' functionalities by using S(N)2 methodology. Antibacterial evaluation of compounds I with A = acetyl, isopropyl, methylthio, methylsulfinyl, methylsulfonyl, and sulfonamido and a variety of different 'B' groups against Staphylococcus aureus and Enterococcus faecalis concluded that the compounds with B = aminoacyl, and particularly acetamido, were the most active of those examined in each A series, possessing MICs in the range of 0.5-4 μg/mL for the most active compounds described.
