726196-75-4

Upstream product

• 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 
• 726196-69-6 5-(4-(benzyloxy)phenyl)-1-(4-methoxyphenyl)-3-(2,2,2-trifluoroethoxy)-1H-1,2,4-triazole 

Downstream Products

• 524699-85-2 1,5-bis(4-methoxyphenyl)-3-(2,2,2-trifluoroethoxy)-1H-1,2,4-triazole 

Relevant academic research and scientific papers

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.

IMIDAZOLE AND TRIAZOLE DERIVATIVES USEFUL AS SELECTIVE COX-1 INHIBITORS

A compound of the formula (I): or salts thereof, which are useful for treatment and/or prevention of inflammatory conditions, various pains, collagen diseases, autoimmune diseases, thrombosis, cancer or neurodengenerative diseases.