524699-85-2

Upstream product

• 99793-84-7 1,5-bis(4-methoxyphenyl)-1H-1,2,4-triazol-3-ol 
• 353-83-3 1,1,1-trifluoro-2-iodoethane 
• 100-07-2 4-methoxy-benzoyl chloride 
• 524699-71-6 2-(4-methoxybenzoyl)-2-(4-methoxyphenyl)hydrazine-1-carboxamide 
• 726196-77-6 5-(4-(benzyloxy)phenyl)-1-(4-methoxyphenyl)-1H-1,2,4-triazol-3-ol 
• 726196-76-5 2-(4-(benzyloxy)benzoyl)-2-(4-methoxyphenyl)-hydrazinecarboxamide 
• 1486-50-6 4-(benzyloxy)benzoic acid chloride 
• 101935-25-5 2-(4-methoxyphenyl)hydrazine-1-carboxamide 
• 726196-75-4 4-(1-(4-methoxyphenyl)-3-(2,2,2-trifluoroethoxy)-1H-1,2,4-triazol-5-yl)phenol 
• 74-88-4 methyl iodide 
• 726196-69-6 5-(4-(benzyloxy)phenyl)-1-(4-methoxyphenyl)-3-(2,2,2-trifluoroethoxy)-1H-1,2,4-triazole 

Relevant academic research and scientific papers

Synthesis of [18F]PS13 and evaluation as a PET radioligand for cyclooxygenase-1 in monkey

Cyclooxygenase-1 (COX-1) and its isozyme COX-2 are key enzymes in the syntheses of prostanoids. Imaging of COX-1 and COX-2 selective radioligands with positron emission tomography (PET) may clarify how these enzymes are involved in inflammatory conditions

3-Substituted 1,5-Diaryl-1H-1,2,4-triazoles as Prospective PET Radioligands for Imaging Brain COX-1 in Monkey. Part 1: Synthesis and Pharmacology

Cyclooxygenase-1 (COX-1) is a key enzyme in the biosynthesis of proinflammatory thromboxanes and prostaglandins and is found in glial and neuronal cells within brain. COX-1 expression is implicated in numerous neuroinflammatory states. We aim to find a direct-acting PET radioligand for imaging COX-1 in human brain as a potential biomarker of neuroinflammation and for serving as a tool in drug development. Seventeen 3-substituted 1,5-diaryl-1H-1,2,4-triazoles were prepared as prospective COX-1 PET radioligands. From this set, three 1,5 (4-methoxyphenyl)-1H-1,2,4-triazoles, carrying a 3-methoxy (5), 3 (1,1,1 trifluoroethoxy) (20), or 3-fluoromethoxy substituent (6), were selected for radioligand development, based mainly on their high affinities and selectivities for inhibiting human COX-1, absence of carboxyl group, moderate computed lipophilicities, and scope for radiolabeling with carbon-11 (t1/2 = 20.4 min) or fluorine-18 (t1/2 = 109.8 min). Methods were developed for producing [11C]5, [11C]20, and [d2-18F]6 from hydroxy precursors in a form ready for intravenous injection for prospective evaluation in monkey with PET.

Triazole derivatives

A compound of the formula (I): wherein R1 is lower alkyl which is optionally substituted with halogen, cyano, N,N-di(lower)alkylcarbamoyl, phenyl optionally substituted with halogen, or heterocyclic group, cyclo(lower)alkyl, lower alkynyl, or N