Related Experiment Video
Updated: Oct 1, 2026
![Solid-phase Synthesis of [4.4] Spirocyclic Oximes](/_next/image?url=https%3A%2F%2Fcloudfront.jove.com%2FCDNSource%2Fteasers%2F58508.jpg&w=3840&q=50)
Solid-phase Synthesis of [4.4] Spirocyclic Oximes
Published on: February 6, 2019
Novel piperidinyloxy oxazolidinone antibacterial agents. Diversification of the N-Substituent
Michele A Weidner-Wells1, Christine M Boggs, Barbara D Foleno
1Antimicrobial Agents Research Team, Johnson and Johnson Pharmaceutical Research and Development, LLC, 1000 Route 202, Raritan, NJ 08869, USA. mwells@prdus.jnj.com
Abstract:
Oxazolidinone antibacterial agents, where the morpholino group of linezolid was replaced with an N-substituted piperidinyloxy moiety, were synthesized and shown to be active against a variety of resistant and susceptible Gram-positive organisms. The functionality attached to the piperidine nitrogen was varied extensively to determine the SAR for this series. One of the most potent compounds, 11, showed in vivo efficacy upon subcutaneous administration in a Staphylococcus aureus Smith murine systemic infection.
Related Concept Videos
Inhibitors of Bacterial DNA Synthesis
Directing and Steric Effects in Disubstituted Benzene Derivatives
Combined Effects of Drugs: Synergism
Such synergistic combinations...
Nucleophilic Aromatic Substitution of Aryldiazonium Salts: Aromatic SN1
In the Sandmeyer reaction, for example, the diazonio group is replaced by a chloro, bromo, or cyano...
ortho–para-Directing Activators: –CH3, –OH, –⁠NH2, –OCH3
Inhibitors of Bacterial Protein Synthesis
