Phenyl Substituted 4-Hydroxypyridazin-3(2H)-ones and 5-Hydroxypyrimidin-4(3H)-ones: Inhibitors of Influenza A Endonuclease

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Phenyl Substituted 4-Hydroxypyridazin-3(2H)-ones and 5-Hydroxypyrimidin-4(3H)-ones: Inhibitors of Influenza A Endonuclease

Seasonal and pandemic influenza outbreaks remain a major human health problem. Inhibition of the endonuclease activity of influenza RNA-dependent RNA polymerase is attractive for the development of new agents for the treatment of influenza infection. Our earlier studies identified a series of 5- and 6-phenyl substituted 3-hydroxypyridin-2(1H)-ones that were effective inhibitors of influenza end...

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Synthesis, antiviral and cytotoxic investigation of 2-phenyl-3-substituted quinazolin-4(3H)-ones.

OBJECTIVES A series of 3(benzylideneamino)-2-phenyl quinazoline-4(3H)-ones was synthesized by reaction of 3-amino-2-phenyl-3H-quinazoline-4-one with various carbonyl compounds. MATERIALS AND METHODS Chemical structures of the synthesized compounds were confirmed by IR, 1H-NMR and mass spectral analysis. Title compounds were investigated for cytotoxicity and antiviral activity against herpes s...

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Crystal structures of three substituted 3-aryl-2-phenyl-2,3-di­hydro-4H-1,3-benzo­thia­zin-4-ones

Three ring-substituted 3-aryl analogs of 2-phenyl-2,3-di-hydro-4H-1,3-benzo-thia-zin-4-one, namely 3-(4-meth-oxy-phen-yl)-2-phenyl-4H-1,3-benzo-thia-zin-4-one, C21H17NO2S, (I), 2-phenyl-3-[4-(tri-fluoro-meth-yl)phen-yl]-2,3-di-hydro-4H-1,3-benzo-thia-zin-4-one toluene hemisolvate, C21H14F3NOS·0.5C7H8, (II), and 3-(3-bromo-phen-yl)-2-phenyl-2,3-di-hydro-4H-1,3-benzo-thia-zin-4-one toluene hemiso...

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Synthesis and pharmacological activity of 2-(2-substituted-phenyl)-3-(4-{1-[2- (1H-tetrazol-5-yl)-biphenyl-4-ylmethyl])-1H-benzoimidazol-2-yl}-phenyl)- thiazolidin-4-ones

An easy and efficient method to obtain Schiff bases of [2-(2-substituted-phenyl)-3-(4-{1-[2-(1Htetrazol-5-yl)-biphenyl-4-ylmethyl])-1H benzoimidazol-2-yl}-phenyl)thiazolidin-4-one] using different aromatic aldehydes. Reaction mixture of Schiff base (0.01 mol) and mercaptoacetic acid (0.05 mol) dissolved in dioxane (50 ml), anhydrous zinc chloride (0.008 mol) was added and refluxed for 12 hrs. T...

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A comparative QSAR study of aryl-substituted isobenzofuran-1(3H)-ones inhibitors

A comparative workflow, including linear and non-linear QSAR models, was carried out to evaluate the predictive accuracy of models and predict the inhibition activity of a series of aryl-substituted isobenzofuran-1(3H)-ones. The data set consisted of 34 compounds was classified into the training and test sets, randomly. Molecular descriptors were selected using the genetic algorithm (GA) as a f...

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ژورنال

عنوان ژورنال: Journal of Medicinal Chemistry

سال: 2014

ISSN: 0022-2623,1520-4804

DOI: 10.1021/jm500958x