- Synthesis and antiviral activity of new 4-(phenylamino)thieno[2,3-b] pyridine derivatives
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Several new 4-(phenylamino)thieno[2,3-6]pyridines (6a-e) were synthesized and tested against herpes simplex virus type 1 (HSV-1). For the first time one compound (6a) of this heterocyclic system showed 86% of inhibitory indicating that these compounds retain antiviral potency in comparison to the parent pirazolo-pyridine derivatives.
- Bernardino, Alice M. R.,Pinheiro, Luiz C. S.,Ferreira, Vitor Francisco,Azevedo, Alexandre R.,Carneiro, Jose W. De M.,Souza, Thiago M. L.,Frugulhetti, Izabel C. P. P.
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- Heterocyclic fused pyridone carboxylic acid M1 positive allosteric modulators
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The phenyl ring in a series of quinolone carboxylic acid M1 positive allosteric modulators was replaced with a variety of heterocycles in order to reduce protein plasma binding and enhance CNS exposure.
- Kuduk, Scott D.,Di Marco, Christina N.,Chang, Ronald K.,Ray, William J.,Ma, Lei,Wittmann, Marion,Seager, Matthew A.,Koeplinger, Kenneth A.,Thompson, Charles D.,Hartman, George D.,Bilodeau, Mark T.
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scheme or table
p. 2533 - 2537
(2010/08/05)
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- 4-Oxo-4,7-dihydrothieno[2,3-b]pyridines as non-nucleoside inhibitors of human cytomegalovirus and related herpesvirus polymerases
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A novel series of 4-oxo-4,7-dihydrothieno[2,3-6]pyridine-5-carboxamides have been identified as potential antivirals against human herpesvirus infections resulting from human cytomegalovirus (HCMV), herpes simplex virus type 1 (HSV-1), and varicella-zoster virus (VZV). Compounds 10c and 14 demonstrated broad-spectrum inhibition of the herpesvirus polymerases HCMV, HSV-1, and VZV. High specificity for the viral polymerases was observed compared to human α polymerase. The antiviral activity of 10c and 14, as determined by plaque reduction assay, was comparable or superior to that of existing antiherpes drugs, ganciclovir (for HCMV) and acyclovir (for HSV-1 and VZV). Drug resistance to compound 14 correlated to point mutations in conserved domain III of the herpesvirus DNA polymerase, but these mutations do not confer resistance to existing nucleoside therapy. In addition, compound 14 maintained potent antiviral activity against acyclovir-resistant HSV-1 strains. Substitution to the pyridone nitrogen (N7) was found to be critical for enhanced in vitro antiviral activity.
- Schnute, Mark E.,Cudahy, Michele M.,Brideau, Roger J.,Homa, Fred L.,Hopkins, Todd A.,Knechtel, Mary L.,Oien, Nancee L.,Pitts, Thomas W.,Poorman, Roger A.,Wathen, Michael W.,Wieber, Janet L.
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p. 5794 - 5804
(2007/10/03)
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- Glucocorticoid mimetics, methods of making them, pharmaceutical compositions and uses thereof
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Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6 and X are as defined herein for Formula (IA) and Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
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Page/Page column 44
(2008/06/13)
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- HETEROARYL-ETHANOLAMINE DERIVATIVES AS ANTIVIRAL AGENTS
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The present invention provides a compound of formula (I), which are useful as antiviral agents, in particular, as agents against viruses of the herpes family.
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