501008-39-5

Upstream product

• 105-36-2 ethyl bromoacetate 
• 626-43-7 3,5-Dichloroaniline 

Downstream Products

• 1419030-74-2 C₁₁H₁₁Cl₂NO 
• 1225761-30-7 N-allyl-3,5-dichloroaniline 
• 1419030-78-6 ethyl 2-(allyl(3,5-dichlorophenyl)amino)acetate 
• 42288-29-9 2-((3,5-dichlorophenyl)arnino)acetic acid 
• 1426318-90-2 ethyl (2R,3S)-2-(3,5-dichlorophenylamino)-3-hydroxy-4-oxo-4-phenylbutanoate 

Relevant academic research and scientific papers

A novel synthesis of 1-aryl-3-piperidone derivatives

A novel method to construct the 1-aryl-3-piperidone scaffold is described here. Starting from 3,5-dichloroaniline, a seven-step synthesis, without the use of protecting groups, generates the desired 3-piperidone ring in an overall yield of 30% through a key Morita-Baylis-Hillman reaction and ring-closing metathesis, providing easy access to diverse and useful heterocycles.

1,3,4,9-TETRAHYDRO-2H-PYRIDO[3,4-B]INDOLE DERIVATIVE COMPOUNDS AND USES THEREOF

The present invention relates to 1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indole derivative compounds and uses thereof. In particular, compounds of the invention have antibacterial activity and/or are capable of re-sensitizing methicillin-resistant Staphylococcus aureus to a P-lactam antibiotic or a combination of a P-lactam antibiotic and a P-lactamase inhibitor. The present invention also relates to a method for producing and using said compounds.

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.

SPECIFIC INHIBITORS OF METHIONYL-TRNA SYNTHETASE

The present disclosure is generally directed to compositions useful in the inhibition of MetRS and methods for treating diseases that are ameliorated by the inhibition of MetRS.