- 5,6-DIHYDRO-1H-PYRIDIN-2-ONE COMPOUNDS
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The invention is directed to 5,6-dihydro-lH-pyridin-2-one compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.
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- Synthesis of pyrido-1,2,4-thiadiazines related to antihypertensive 1,2,4-benzothiadiazine-1,1-dioxides
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Oxidation of 3-phenyl-2H-pyrido[2,3-e]-1,2,4-thiadiazine with sodium hypochlorite and, separately, m-chloroperoxybenzoic acid afforded a 1,1- dioxide and a 5-oxide derivative, respectively. Further examples of such 1,1- dioxide derivatives were synthesised by treating 2-amino-5-methylpyridine with orthoesters and these were subsequently oxidised to novel 1,1,5- trioxides. A short route has been developed for the synthesis of 4- aminopyridine-3-sulfonamide which was used for the preparation of 4H- pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxides; oxidation of the parent member of the series gave a 1,1,7-trioxide derivative. 3-Aminopyridine-4-sulfonamide has been prepared, and then condensed with triethyl orthoformate to afford 4H-pyrido[3,4-e]-1,2,4-thiadiazine 1,1-dioxide.
- Neill, Colin G.,Preston, Peter N.,Wightman, Richard H.
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p. 13645 - 13654
(2007/10/03)
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- Studies on Anticoccidial Agents. 13. Synthesis and Anticoccidial Activity of Nitropyridine-2- and -3-sulfonamides and Derivatives
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Eight nitropyridinesulfonamides andd pyridinesulfonamide N-oxides as their bioisosteres were prepared and evaluated for anticoccidial activity.Of these compounds, 2-, 4- and 5-nitropyridine-3-sulfonamides and pyridine-2- and -3-sulfonamide N-oxides were found to be active against Eimeria tenella.Thus, the relative positions, ortho or meta, of the substituents in nitropyridine-3-sulfonamides and pyridinesulfonamide N-oxides are important for anticoccidial activity.N-Substituted analogues of 5-nitropyridine-3-sulfonamide were also prepared and optimal anticoccidial activity was attained with the sulfonamide and its lower N-alkyl derivatives.The mode of action of 5-nitropyridine-3-sulfonamide was examined and found to be active in the sporozoite and the first schizogony stages.
- Morisawa, Yasuhiro,Kataoka, Mitsuru,Nagahori, Hitoshi,Sakamoto, Toshiaki,Kitano, Noritoshi,et al.
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p. 1376 - 1380
(2007/10/02)
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