65141-27-7

Upstream product

• 1885-14-9 phenyl chloroformate 
• 6315-89-5 3,4-dimethoxyaniline 
• 37527-66-5 3,4-dimethoxyphenylisocyanate 
• 108-95-2 phenol 

Downstream Products

• 788795-18-6 4-(3,4-methoxyphenyl)semicarbazide 
• 415692-67-0 N-(3,4-dimethoxy-phenyl)-4-methyl-benzamide 
• 1610766-80-7 (2R)-1-cyanobutan-2-yl-[(1S)-1-(3-{[(3,4-dimethoxyphenyl)carbamoyl]amino}phenyl)ethyl] carbamate 

Relevant academic research and scientific papers

N-(3,5-dimethyladamantane-1-yl)-N'-substituted phenylurea compound as well as preparation method and application thereof

The invention belongs to the technical field of medicinal chemistry, in particular to N-(3,5-dimethyladamantane-1-yl)-N'-substituted phenylurea compounds as well as preparation methods and application thereof. The compounds have the structure shown in the formula I. The compounds are proved that the compounds can improve the image recognition memory, the working and learning memory, the spatial learning and memory ability of model rats and has good anti-alzheimer effects by the new object discrimination experiments, Y-maze experiments, positioning navigation and space exploration experiments in mats. The formula I is shown in the description.

Design, synthesis and biological evaluation of novel inosine 5′-monophosphate dehydrogenase (IMPDH) inhibitors

This study is based on our attempts to further explore the structure-activity relationship (SAR) of VX-148 (3) in an attempt to identify inosine 5′-mono-phosphate dehydrogenase (IMPDH) inhibitors superior to mycophenolic acid. A five-point pharmacophore developed using structurally diverse, known IMPDH inhibitors guided further design of novel analogs of 3. Several conventional as well as novel medicinal chemistry strategies were tried. The combined structure- and ligand-based approaches culminated in a few analogs with either retained or slightly higher potency. The compounds which retained the potency were also checked for their ability to inhibit human peripheral blood mononuclear cells proliferation. This study illuminates the stringent structural requirements and strict SAR for IMPDH II inhibition.

Synthesis and biological evaluation of 4-phenoxy-6,7-disubstituted quinolines possessing semicarbazone scaffolds as selective c-Met inhibitors

Novel quinoline derivatives bearing acyclic semicarbazones were prepared and their chemical structures as well as the relative stereochemistry were confirmed. All the synthesized compounds were evaluated for their c-Met kinase inhibitory activity and their cytotoxicity against the cell lines HT-29, MKN-45, and MDA-MB-231 in vitro. Several potent compounds were further evaluated against A549 cells. Most compounds displayed moderate to excellent activity, and the structure-activity relationship studies identified the most promising compound 35 as a selective c-Met kinase inhibitor (IC50 = 4.3 nM). Compound 35 showed a 3.5- and 18.8-fold increase in cytotoxicity in vitro against HT-29 and A549 cells, respectively, compared to that of foretinib. Poor off-target effects of compound 35 were further confirmed by the antiproliferative activity against the c-Met inhibition less sensitive MDA-MB-231 cell line (IC50 = 0.77 μM). Copyright

A simple method for the preparation of di-, tri- and tetrasubstituted non-symmetrical ureas

The synthesis of a series of di-, tri- and tetrasubstituted non-symmetrical ureas is described. Di- and trisubstituted ureas are prepared in excellent yield by treatment of a phenyl carbamate in a self-tunable single-mode microwave synthesizer with a primary or secondary amine. The synthetically more challenging tetrasubstituted urea can be prepared using the 4-nitrophenyl carbamate and a secondary amine. Georg Thieme Verlag Stuttgart.