- Thiazolides as novel antiviral agents. 1. Inhibition of hepatitis B virus replication
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We report the syntheses and activities of a wide range of thiazolides [viz., 2-hydroxyaroyl-N-(thiazol-2-yl)amides] against hepatitis B virus replication, with QSAR analysis of our results. The prototypical thiazolide, nitazoxanide [2-hydroxybenzoyl-N-(5-
- Stachulski, Andrew V.,Pidathala, Chandrakala,Row, Eleanor C.,Sharma, Raman,Berry, Neil G.,Iqbal, Mazhar,Bentley, Joanne,Allman, Sarah A.,Edwards, Geoffrey,Helm, Alison,Hellier, Jennifer,Korba, Brent E.,Semple, J. Edward,Rossignol, Jean-Francois
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scheme or table
p. 4119 - 4132
(2011/08/05)
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- ACYLAMINOTHIAZOLE DERIVATIVES AND USE THEREOF AS BETA-AMYLOID INHIBITORS
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Compounds of formula (I) as defined herein: inhibit the formation of the β-amyloid peptide (β-A4) and are, therefore, useful in the treatment of pathologies in which a β-amyloid peptide (β-A4) formation inhibitor provides a therapeutic benefit. Particular
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Page/Page column 13-14
(2010/11/25)
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- BROADSPECTRUM SUBSTITUTED BENZISOXAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS
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The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs esters and metabolites thereof.It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with another anti-retroviral agent, and to their use in assays as reference compounds or as reagents.
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Page/Page column 26
(2008/06/13)
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- Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors
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PCT No. PCT/US94/09139 Sec. 371 Date Jan. 24, 1996 Sec. 102(e) Date Jan. 24, 1996 PCT Filed Aug. 23, 1994 PCT Pub. No. WO95/06030 PCT Pub. Date Mar. 2, 1995The invention relates to sulfonamide-containing hydroxyethylamine protease inhibitor compounds, their process of making, composition and method of use for inhibiting retroviral proteases such as human immunodeficiency virus.
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- Studies on Decarboxylation Reactions. Part 7. Kinetic Study of the Decarboxylation of 2-Amino- and 2-Phenylamino-thiazole-5-carboxylic Acids
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The rate constants of the decarboxylation reaction of 2-amino- and 2-phenylamino-thiazole-5-carboxylic acid (3a-b), and, for comparison, of 5-phenylamino-1,3,4-thiadiazole-2-carboxylic acid (2b) have been measured in water over a range of proton activities.The results obtained suggest: (i) compound 2b decarboxylates, in the whole range of proton activity studied, through a unimolecular decarboxyprotonation mechanism characteristic of 1,3,4-oxa- and 1,3,4-thiadiazole derivatives; (ii) in contrast, 3a-b decarboxylate via either a unimolecular decarboxyprotonation or a bimolecular protiodecarboxylation mechanism as a function of proton activity.
- Noto, Renato,Ciofalo, Maurizio,Buccheri, Francesco,Werber, Guiseppe,Spinelli, Domenico
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p. 349 - 352
(2007/10/02)
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