3589-58-0

Upstream product

• 105-39-5 chloroacetic acid ethyl ester 
• 99-09-2 3-nitro-aniline 
• 105-36-2 ethyl bromoacetate 
• 623-73-4 diazoacetic acid ethyl ester 
• 10242-06-5 (R/S)-(3-nitrophenyl)glycine 
• 64-17-5 ethanol 

Downstream Products

• 1007598-83-5 (3-nitro-phenyl-N-(t-butylaminosulfonyl)amino)-acetic acid ethyl ester 
• 139677-65-9 2-((3-nitrophenyl)amino)acetohydrazide 
• 140373-78-0 2-amino-2-(3-nitrophenyl)-1-ethanol 

Relevant academic research and scientific papers

Arylamino containing hydroxamic acids as potent urease inhibitors for the treatment of Helicobacter pylori infection

A novel series of aniline-containing hydroxamic acids were designed, synthesized and evaluated as anti-virulence agents for the treatment of gastritis and gastric ulcer caused by Helicobacter pylori. In vitro enzyme-based screen together with in vivo assays and structure?activity relationship (SAR) studies led to the discovery of three potent urease inhibitors 3-(3,5-dichlorophenylamino)–N-hydroxypropanamide (3a), 3-(2-chlorophenylamino)–N-hydroxypropanamide (3d) and 3-(2,4-dichlorophenylamino)–N-hydroxypropanamide (3n). Compounds 3a, 3d and 3n showed excellent urease inhibition with IC50 values 0.043 ± 0.005, 0.055 ± 0.008 and 0.018 ± 0.002 μM, and significantly depressed gastritis developing at the dose of 32 mg/kg b. i.d with eradication rates of H. pylori reaching 92.3, 84.6 and 100%, respectively. Preliminary safety studies (acute toxicity in mice) disclosed that 3a, 3d and 3n was well-tolerated in KM mice with LD50s of 2982.8, 3349.4 and 3126.9 mg/kg, respectively. Collectively, the data obtained in this study indicate that 3a, 3d and 3n, in particular 3n, could considered as promising candidates for the potential treatment of H. pylori caused gastritis and gastric ulcer, and hence merit further studies.

Identification, structure modification, and characterization of potential small-molecule SGK3 inhibitors with novel scaffolds

The serum and glucocorticoid-regulated kinase (SGK) family has been implicated in the regulation of many cellular processes downstream of the PI3K pathway. It plays a crucial role in PI3K-mediated tumorigenesis, making it a potential therapeutic target for cancer. SGK family consists of three isoforms (SGK1, SGK2, and SGK3), which have high sequence homology in the kinase domain and similar substrate specificity with the AKT family. In order to identify novel compounds capable of inhibiting SGK3 activity, a high-throughput screening campaign against 50,400 small molecules was conducted using a fluorescence-based kinase assay that has a Z' factor above 0.5. It identified 15 hits (including nitrogen-containing aromatic, flavone, hydrazone, and naphthalene derivatives) with IC50 values in the low micromolar to sub-micromolar range. Four compounds with a similar scaffold (i.e., a hydrazone core) were selected for structural modification and 18 derivatives were synthesized. Molecular modeling was then used to investigate the structure-activity relationship (SAR) and potential protein–ligand interactions. As a result, a series of SGK inhibitors that are active against both SGK1 and SGK3 were developed and important functional groups that control their inhibitory activity identified.

Use of 2-aminothiazoline derivatives as inhibitors of inducible no-synthase

The present invention relates to the use of 2-aminothiazoline derivatives of formula: in which either R1 is a hydrogen atom or an alkyl radical and R2 is an alkyl, -alk-NH2, —CH2—R3, —CH2—S