448233-17-8

Upstream product

• 202598-92-3 phenyl [3-(trifluoromethyl)phenyl]carbamate 
• 98-16-8 3-trifluoromethylaniline 
• 329-01-1 1-isocyanato-3-trifluoromethyl-benzene 

Downstream Products

• 1449478-71-0 3-tert-butyl-5-ethyl-N-(3-(trifluoromethyl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo [4,3-c]pyridine-1-carboxamide 
• 1449478-63-0 5-ethyl-3-methyl-N-(3-(trifluoromethyl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine-1-carboxamide 
• 1449478-51-6 C₁₈H₂₁F₃N₄O 
• 1449478-43-6 C₁₅H₁₅F₃N₄O 
• 527684-72-6 2',3',5'-tri-O-acetyl-2-[3-(3-trifluoromethylphenyl)aminocarbonyltriazene-1-yl]adenosine 

Relevant academic research and scientific papers

Design, Synthesis, and Biological Evaluation of Triazolone Derivatives as Potent PPARα/δDual Agonists for the Treatment of Nonalcoholic Steatohepatitis

Peroxisome proliferator-activator receptors α/δ(PPARα/δ) are regarded as potential therapeutic targets for nonalcoholic steatohepatitis (NASH). However, PPARα/δdual agonist GFT-505 exhibited poor anti-NASH effects in a phase III clinical trial, probably due to its weak PPARα/δagonistic activity and poor metabolic stability. Other reported PPARα/δdual agonists either exhibited limited potency or had unbalanced PPARα/δagonistic activity. Herein, we report a series of novel triazolone derivatives as PPARα/δdual agonists. Among them, compound H11 exhibited potent and well-balanced PPARα/δagonistic activity (PPARα EC50 = 7.0 nM; PPARδEC50 = 8.4 nM) and a high selectivity over PPARγ(PPARγEC50 = 1316.1 nM) in PPAR transactivation assays. The crystal structure of PPARδin complex with H11 revealed a unique PPARδ-agonist interaction. H11, which had excellent PK properties and a good safety profile, showed potent in vivo anti-NASH effects in preclinical models. Together, H11 holds a great promise for treating NASH or other inflammatory and fibrotic diseases.

Synthesis, In-vitro evaluation and molecular docking studies of oxoindolin phenylhydrazine carboxamides as potent and selective inhibitors of ectonucleoside triphosphate diphosphohydrolase (NTPDase)

Members of the ectonucleoside triphosphate diphosphohydrolases (NTPDases) constitute the major family of enzymes responsible for the maintenance of extracellular levels of nucleotides and nucleosides by catalyzing the hydrolysis of nucleoside triphosphate

Synthetic method of medical intermediate semi-carboamidrazone

The invention discloses a synthesis method of medical intermediate semicarbazone. According to a method, the semicarbazone is synthesized by taking dichloroethane, triphosgene, m-trifluoromethyl aniline, phenyl isonitrile, hydrazine hydrate, N-(3-trifluoromethyl phenyl)-semicarbazide and thiophene-2-formaldehyde as main raw materials and using the N-(3-trifluoromethyl phenyl)-semicarbazide. Aftersulfo group modified-SZ@SBA-15-SO3H catalyst is added, thiophene-2-formaldehyde is added, so that sediments are produced immediately; a thiophene ring is a five-atom and six-electron conjugate structure; after thiophene-2-formaldehyde-N(4)-m-trifluoromethyl phenyl semicarbazone is generated under the catalytic action, as -CN and the thiophene ring form conjugation, electrons are more dispersive and more stable; the semicarbazone preparation method has the characteristics of simplicity, feasibility, short preparation period and the like; the raw materials and the catalyst which are used in a technological process are high in efficiency, simple, convenient, easy to recycle, regenerable, extremely environmentally friendly and wide in application range, and has an excellent catalysis effect onsemicarbazone synthesis reaction.

N6-cyclopentyl-2-(3-phenylaminocarbonyltriazene-1-yl)adenosine (TCPA), a very selective agonist with high affinity for the human adenosine A1 receptor

Four subtypes of adenosine receptors are currently known, that is, A1, A2A, A2B, and A3 receptors. Interestingly, quite substantial species differences exist especially between human and rat A3 receptors. As a result, ligands such as CCPA, which are very selective for the rat A1 receptor versus the human A3 receptor, are substantially less selective when the human A1 and A3 receptors are compared. New 2-substituted and 2,N6-disubstituted adenosines were synthesized, and their affinities for the human adenosine A1, A2A, A2B, and A3 receptors were determined. Although large substituents on the C2-position are generally thought to yield adenosine A2A receptor selective ligands, the reported series of 2-triazeno-substituted adenosines had a very high affinity for the A1 receptor. For example, 2-(3-phenylaminocarbonyltriazene-1-yl)adenosine had an affinity of 6.1 ± 1.3 nM for the human adenosine A1 receptor. Introduction of a diphenethyl substituent at the N6-position of this compound resulted in a high-affinity agonist, 3.1 ± 0.9 nM, for the human adenosine A1 receptor with 316- and 45-fold selectivity versus the human A2A and human A3 receptors, respectively. The most selective, high-affinity human adenosine A1 receptor agonist was the disubstituted compound N6-cyclopentyl-2-(3-phenylaminocarbonyltriazene-1-yl)adenosine (TCPA). TCPA had an affinity of 2.8 ± 0.8 nM for the human adenosine A1 receptor and was 75-fold and 214-fold selective versus the human A2A and human A3 receptors, respectively. In addition, TCPA was a full agonist and inhibited the forskolin-induced cAMP production of CHO cells stably transfected with the human adenosine A1 receptor with an IC50 of 1.5 ± 0.5 nM.