Synthesis and antibacterial activities of chiral 1,3-oxazinan-2-one derivatives
摘要:
We report here the design, synthesis, and antibacterial activities of novel classes of compounds containing chiral 1,3-oxazinan-2-ones and oxazolidinones as the basic Core Structures. These compounds are tertiary amines containing the core structures and two aryl substituents. Several of these molecules exhibit potent antibacterial activities against the tested Gram-positive bacteria, including Staphylococcus aureus, Enterococcus faecalis, and Bacillus subtilis. These compounds represent new structure scaffolds and can be further optimized to give new antibacterial agents with structures significantly different from those of existing classes of antibiotics. (C) 2006 Elsevier Ltd. All rights reserved.
Synthesis and antibacterial activities of chiral 1,3-oxazinan-2-one derivatives
摘要:
We report here the design, synthesis, and antibacterial activities of novel classes of compounds containing chiral 1,3-oxazinan-2-ones and oxazolidinones as the basic Core Structures. These compounds are tertiary amines containing the core structures and two aryl substituents. Several of these molecules exhibit potent antibacterial activities against the tested Gram-positive bacteria, including Staphylococcus aureus, Enterococcus faecalis, and Bacillus subtilis. These compounds represent new structure scaffolds and can be further optimized to give new antibacterial agents with structures significantly different from those of existing classes of antibiotics. (C) 2006 Elsevier Ltd. All rights reserved.
Process for the preparation of oxazolidinones and method of use thereof
申请人:Hollingsworth I. Rawle
公开号:US20070265451A1
公开(公告)日:2007-11-15
A process for preparing N-(substituted)-C-(substituted methyl)-oxazolidinones, C-(substituted methyl)-oxazolidinones, and N-(substituted)-C-(substituted methyl)-oxazolidinones, preferably chiral, from optically active C-(protected oxymethyl)-oxazolidinones is described. The process can be used to produce combinatorial libraries of the above substituted oxazolidinones in a two or three step reaction comprising a plurality of reagents differing in numbers of carbons or particular substituted oxazolidinones. A number of substituted oxazolidinones produced using the above process have been discovered to have antimicrobial activity.
PROCESS FOR THE PREPARATION OF OXAZOLIDINONES AND METHOD OF USE THEREOF
申请人:Hollingsworth Rawle I.
公开号:US20080146458A1
公开(公告)日:2008-06-19
Substituted oxazolidinone of the formula:
wherein R
2
is alkyl selected from the group consisting of methyl, ethyl, and isopropyl moieties, are described. The compounds are antibacterial.