73883-19-9Relevant academic research and scientific papers
3-Substituted pyrazoles and 4-substituted triazoles as inhibitors of human 15-lipoxygenase-1
Pelcman, Benjamin,Sanin, Andrei,Nilsson, Peter,No, Kiyo,Schaal, Wesley,?hrman, Sara,Krog-Jensen, Christian,Forsell, Pontus,Hallberg, Anders,Larhed, Mats,Boesen, Thomas,Kromann, Hasse,Vogensen, Stine Byskov,Groth, Thomas,Claesson, Hans-Erik
, p. 3024 - 3029 (2015/06/22)
Investigation of 1N-substituted pyrazole-3-carboxanilides as 15-lipoxygenase-1 (15-LOX-1) inhibitors demonstrated that the 1N-substituent was not essential for activity or selectivity. Additional halogen substituents on the pyrazole ring, however, increased activity. Further development led to triazole-4-carboxanilides and 2-(3-pyrazolyl) benzoxazoles, which are potent and selective 15-LOX-1 inhibitors.
PYRAZOLES USEFUL IN THE TREATMENT OF INFLAMMATION
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Page/Page column 45, (2008/06/13)
There is provided compounds of formula (I), wherein R1, R2, X1, X2 and n have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a lipoxygenase (e.g. 15-lipoxygenase) is desired and/or required, and particularly in the treatment of inflammation.
PYRAZOLES USEFUL IN THE TREATMENT OF INFLAMMATION
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Page/Page column 54, (2008/06/13)
There is provided compounds of formula (I), wherein R1, R2, X1, X2 and n have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a lipoxygenase (e.g. 15-lipoxygenase) is desired and/or required, and particularly in the treatment of inflammation.
Fluorocarbon Derivatives of Nitrogen. Part 8. Reactions Between Heteroaromatic N-Imines (N-Iminopyridinium and N-Iminoquinolinium Ylide) and Perfluoropropene, 2H-Pentafluoropropene, Perfluorobut-2-ene, Perfluoro-(2-methylpent-2-ene), Perfluorobut-2-yne, and Perfluoropyridine: Synthesis..
Banks, Ronald E.,Hitchen, Stephen M.
, p. 1593 - 1600 (2007/10/02)
N-Iminopyridinium ylide reacts with perfluoropropene (or 2H-pentafluoropropene) and perfluorobut-2-ene (or perfluorobut-2-yne) to provide 2-fluoro-3-(trifluoromethyl)pyrazolopyridine and 2,3-bis(trifluoromethyl)pyrazolopyridine, respectively; oxidation of these products with aqueous potassium permanganate gives the corresponding pyrazolecarboxylic acids.Perfluoro-(2-methylpent-2-ene) is attacked by N-iminopyridinium ylide to produce 2-(pentafluoroethyl)-3,3-bis(trifluoromethyl)-3,3a-dihydropyrazolopyridine, which can be converted via thermal treatment with tetracyanoethylene into a mixture of 2-(pentafluoroethyl)-3-(trifluoromethyl)pyrazolopyridine and 5-(dicyanomethylene)-2-(pentafluoroethyl)-3,3-bis(trifluoromethyl)-3,5-dihydropyrazolopyridine.N-Iminoquinolinium ylide reacts with perfluoropropene, perfluorobut-2-ene, and perfluoropyridine in hot dimethylformamide in the presence of potassium carbonate to yield 2-fluoro-3-(trifluoromethyl)pyrazoloquinoline, 2,3-bis(trifluoromethyl)pyrazoloquinoline, and N-(tetrafluoro-4-pyridyl)iminoquinolinium ylide, respectively.
