1291068-15-9

Upstream product

• 1012314-40-7 ethyl 4-(4-chlorophenyl)-3-methyl-4-oxydo-2-oxobuten-3-oate lithium salt 
• 368-90-1 4-(trifluoromethyl)phenylhydrazine 
• 169544-41-6 4-(4-chlorophenyl)-3-methyl-2,4-dioxobutyric acid ethyl ester 
• 1291068-13-7 C₂₀H₁₆ClF₃N₂O₂ 
• 1291068-11-5 C₂₀H₁₈ClF₃N₂O₃ 
• 6285-05-8 4'-chloropropiophenone 

Downstream Products

• 1291068-17-1 C₁₈H₁₁Cl₂F₃N₂O 
• 1291068-00-2 5-(4-chlorophenyl)-4-methyl-1-[4-(trifluoromethyl)phenyl]-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide 
• 1291068-01-3 5-(4-chlorophenyl)-4-methyl-1-[4-(trifluoromethyl)phenyl]-N-(azepan-1-yl)-1H-pyrazole-3-carboxamide 
• 1291068-02-4 5-(4-chlorophenyl)-4-methyl-1-[4-(trifluoromethyl)phenyl]-N-(4-methylcyclohexyl)-1H-pyrazole-3-carboxamide 

Relevant academic research and scientific papers

1,5-Diarylpyrazole and vanillin hybrids: Synthesis, biological activity and DFT studies

Herein, we report the design and synthesis of 13 diarylpyrazole hybrids with vanillin constructed as dual compounds against oxidative stress and diabetes. Compounds were tested in two different antioxidant assays. It was found that all compounds showed an

Synthesis, hypoglycemic activity and molecular modeling studies of pyrazole-3-carbohydrazides designed by a CoMFA model

Diabetes and obesity are two universal health problems that constitute a research objective of several groups due to the lack of efficient and safe drug treatment. In this sense, cannabinoid receptor 1 (CB1) has attracted interest because of its role in food intake and metabolic balance, two targets in the control of metabolic syndrome. In this work, novel 1,5-diaryl pyrazole derivatives were synthesized in accordance with the pKi prediction of a previously reported CoMFA model by our group. To further investigate the biological activity of these compounds in metabolic disorders, their hypoglycemic activity in an in vivo model was tested. Interestingly, a high degree of correlation was observed between the predicted pKi and hypoglycemic effect 7 h after administration. Compounds 4, 9 and 13 showed the most significant plasma glucose reduction with decreases of 60%, 64% and 60% respectively. This result not only surpasses the activity of the lead rimonabant, but also that of the reference drug glibenclamide. Moreover, PASS prediction and molecular docking in an excellent validated homology model of CB1 suggest that these compounds would probably act as CB1 antagonists/inverse agonists and therefore, anti-obesity agents. The ligand-receptor complexes demonstrate that 1,5-diaryl pyrazole derivatives bind to the proposed binding site where a hydrophobic moiety interacts with the phenyl rings in the pyrazole nucleus and Lys192 forms a hydrogen bond with the oxygen of the carbonyl group. Dynamics simulations were also carried out to study the stability of the ligand-receptor complexes where the most active compounds showed smaller ΔG values and more hydrogen bonds throughout the simulation. These compounds are considered useful leads for further optimization in the treatment of such metabolic illnesses.

Design, synthesis and biological evaluation of CB1 cannabinoid receptor ligands derived from the 1,5-diarylpyrazole scaffold

The CB1 receptor belongs to the G-protein-coupled receptor superfamily. CB1 antagonism has been considered as a new therapeutic target for the treatment of obesity. In this study, we report the synthesis and in vitro binding affinity assay of some 1,5-dia