Kurasaki, Haruaki published the artcileLpxC Inhibitors: Design, Synthesis, and Biological Evaluation of Oxazolidinones as Gram-negative Antibacterial Agents, Synthetic Route of 105752-04-3, the main research area is oxazolidinone derivative preparation LpxC inhibitor antibacterial; Antibacterial; Gram-negative bacteria; LpxC; oxazolidinone; scaffold hopping.
Herein we report a scaffold-hopping approach to identify a new scaffold with a zinc binding headgroup. Structural information was used to give novel oxazolidinone-based LpxC inhibitors. In particular, the most potent compound, 23j, showed a low efflux ratio, nanomolar potencies against E. coli LpxC enzyme, and excellent antibacterial activity against E. coli and K. pneumoniae. Computational docking was used to predict the interaction between 23j and E. coli LpxC, suggesting that the interactions with C207 and C63 contribute to the strong activity. These results provide new insights into the design of next-generation LpxC inhibitors.
ACS Medicinal Chemistry Letters published new progress about Antibacterial agents. 105752-04-3 belongs to class iodides-buliding-blocks, name is 4-Iodo-3-nitroaniline, and the molecular formula is C6H5IN2O2, Synthetic Route of 105752-04-3.
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com