22036-26-6

Usage

Uses

Used in Pharmaceutical Industry:
3-(4-aminophenyl)-1,3-oxazolidin-2-one is used as a reactant for the preparation of N-phenyl-4,5-dibromopyrrolamides and N-phenylindolamides. These compounds serve as ATPase inhibitors of DNA gyrase, which is an essential enzyme in bacterial DNA replication. Inhibiting DNA gyrase can lead to the disruption of bacterial DNA replication, making these compounds potential candidates for the development of new antibiotics.
Additionally, the compound may have other applications in the synthesis of various pharmaceuticals and bioactive molecules, given its reactivity and structural features. Further research and development are necessary to explore and validate its potential in other areas of the pharmaceutical industry.

Upstream product

• 5198-52-7 3-(4-nitrophenyl)-2-oxazolidinone 
• 586-78-7 para-nitrophenyl bromide 
• 100-01-6 4-nitro-aniline 
• 60480-06-0 1-chloro-2-(4-nitro-phenylcarbamoyloxy)-ethane 

Downstream Products

• 22036-36-8 3-{4-[bis-(2-hydroxy-ethyl)-amino]-phenyl}-oxazolidin-2-one 
• 20406-73-9 [4-(2-oxo-oxazolidin-3-yl)-phenyl]-carbamic acid ethyl ester 
• 1215126-65-0 3-(4-{[4-chloro-5-(trifluoromethyl)pyrimidin-2-yl]amino}phenyl)-1,3-oxazolidin-2-one 
• 22036-37-9 3-{4-[bis-(2-chloro-ethyl)-amino]-phenyl}-oxazolidin-2-one 
• 31847-13-9 3-(4-{4-[bis-(2-chloro-ethyl)-amino]-2,5-dimethoxy-benzylideneamino}-phenyl)-oxazolidin-2-one 
• 20406-71-7 3-[4-(2,2-dichloro-acetylamino)-phenyl]-oxazolidin-2-one 

Relevant academic research and scientific papers

New N-phenyl-4,5-dibromopyrrolamides and N-Phenylindolamides as ATPase inhibitors of DNA gyrase

Following the withdrawal of novobiocin, the introduction of a new ATPase inhibitor of DNA gyrase to the clinic would add the first representative of this mechanistic class to the antibacterial pipeline. This would be of great importance because of the well-known problems associated with antibacterial resistance. Using structure-based design and starting from the recently determined crystal structure of the N-phenyl-4,5-dibromopyrrolamide inhibitor-DNA gyrase B complex, we have prepared 28 new N-phenyl-4,5-dibromopyrrolamides and N-phenylindolamides and evaluated them against DNA gyrase from Escherichia coli. The most potent compound was 2-((4-(4,5-dibromo-1H-pyrrole-2-carboxamido)phenyl)amino)-2-oxoacetic acid (9a), with an IC50 of 0.18 μM against E. coli gyrase. A selected set of compounds was evaluated against DNA gyrase from Staphylococcus aureus and against topoisomerase IV from E. coli and S. aureus, but the activities were weaker. The binding affinity of 2-((4-(4,5-dibromo-1H-pyrrole-2-carboxamido)phenyl)amino)-2-oxoacetic acid (9a) to E. coli gyrase was studied using surface plasmon resonance. In the design of the present series, the focus was on the optimisation of biological activities of compounds - especially by varying their size, the position and orientation of key functional groups, and their acid-base properties. The structure-activity relationship (SAR) was examined and the results were rationalised with molecular docking.

Pyrrole inhibitors of S-nitrosoglutathione reductase as therapeutic agents

The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.

1H-IMIDAZO[4,5-C]QUINOLINE DERIVATIVES IN THE TREATMENT OF PROTEIN KINASE DEPENDENT DISEASES

The invention relates to the use of imidazoquinolines and salts thereof in the treatment of protein kinase diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases, imidazoquinolines for use in the treatment of protein kinase dependent diseases, a method of treatment against said diseases, comprising administering the imidazoquinolines to a warm-blooded animal, especially a human, pharmaceutical preparations comprising an imidazoquinoline, especially for the treatment of a protein kinase dependent disease, novel imidazoquinolines, and a process for the preparation of the novel imidazoquinolines.