925151-32-2

Upstream product

• 111-49-9 hexamethylene imine 
• 201230-82-2 carbon monoxide 
• 619-44-3 methyl 4-iodobenzoate 
• 7377-26-6 4-Methoxycarbonylbenzoyl chloride 

Downstream Products

• 1020664-23-6 4-(azepane-1-ylcarbonyl)benzoic acid 

Relevant academic research and scientific papers

Discovery of Novel Thiophene-arylamide Derivatives as DprE1 Inhibitors with Potent Antimycobacterial Activities

In this study, we report the design and synthesis of a series of novel thiophene-arylamide compounds derived from the noncovalent decaprenylphosphoryl-β-d-ribose 2′-epimerase (DprE1) inhibitor TCA1 through a structure-based scaffold hopping strategy. Systematic optimization of the two side chains flanking the thiophene core led to new lead compounds bearing a thiophene-arylamide scaffold with potent antimycobacterial activity and low cytotoxicity. Compounds 23j, 24f, 25a, and 25b exhibited potent in vitro activity against both drug-susceptible (minimum inhibitory concentration (MIC) = 0.02-0.12 μg/mL) and drug-resistant (MIC = 0.031-0.24 μg/mL) tuberculosis strains while retaining potent DprE1 inhibition (half maximal inhibitory concentration (IC50) = 0.2-0.9 μg/mL) and good intracellular antimycobacterial activity. In addition, these compounds showed good hepatocyte stability and low inhibition of the human ether-à-go-go related gene (hERG) channel. The representative compound 25a with acceptable pharmacokinetic property demonstrated significant bactericidal activity in an acute mouse model of tuberculosis. Moreover, the molecular docking study of template compound 23j provides new insight into the discovery of novel antitubercular agents targeting DprE1.

Diaryl 2- amide-substituted thiophene imide ester compound as well as preparation method and application thereof (by machine translation)

The invention also discloses a 2 - synthesis method thereof, and an application of the compound as an antibacterial agent, in the phthisis-caused by the bacterium, in particular to the, mycobacterium-induced infectious disease (especially (Tuberculosis,TB), mycobacterium- induced mycobacterium, tuberculosis), and (I) the invention, specifically relates to a pharmaceutical composition containing the compound of the present invention or, a R pharmaceutical composition comprising the compound of the present invention. 1 , R2 , R3 , R4 , R5 As described Y in the present invention. as described in the specification, the present invention is directed, to the preparation of novel compounds, having an anti-mycobacterial activity as potential, new drug (s) for the treatment (TB) or preventative treatment of infectious diseases, consisting of M. tuberculosis, in particular phthisis- caused by tubercular mycobacteria, while being useful in overcoming the problems associated with drug resistance. (by machine translation)

Stability or flexibility: Metal nanoparticles supported over cross-linked functional polymers as catalytic active sites for hydrogenation and carbonylation

A novel cross-linked functional polymer was prepared through copolymerization between 1, 3, 4, 6-tetraallylglycoluril and 4-vinyl pyridine. Pt and Pd nanoparticles supported over this polymeric framework (Pt/CFP and Pd/CFP) were detailedly characterized by TEM, EDS, and XPS. Pt nanoparticles were kept in the monodispersed state with the average size of 1.4 nm. Monodispersed Pd nanoparticles were about 4.5 nm. The hydrogenation of nitrobenzenes over Pt/CFP shows high activity and selectivity with the substrate to Pt ratio of 4000 under mild reactions. Pd/CFP was the catalyst for carbonylation of aryl iodides in the presence of secondary amines and acylhydrazines. Double carbonylation with secondary amines produced α-ketoamides with the selectivity of 80%. Diacylhydrazine molecules were synthesized by the direct carbonylation of aryl iodide with acylhydrazine over Pd/CFP. The recyclability and recoverability of Pt/CFP were investigated through a seven-run recycling test of nitrobenzene hydrogenation. The flexibility of Pd/CFP in the carbonylation process was thoroughly explored by a 12-run recycling test. Supported Pt or Pd nanoparticles showed the macroscopic robustness in their catalytic performance in the catalytic cycle. The flexibility of metal nanoparticles and the polymeric supports guaranteed macroscopic catalytic robustness.