- METHODS OF SYNTHESIS AND USE OF CHEMOSPHERES
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The present invention provides, in general, compositions comprising a hydrogel and an agent, for example a therapeutic agent or an imaging agent, for locoregional delivery. In certain preferred embodiments of the invention, the hydrogel compositions are detectable by Magnetic Responance and CT Scan and are used for locoregional delivery of therapeutic agents, for example chemotherapeutic agents. The invention also features polymer matrix compositions comprising nanoparticles that can be loaded after polymerization with bioactive agents, for example a diagnostic agent or therapeutic agent.
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- Metal-mediated inhibition of escherichia coli methionine aminopeptidase: Structure-activity relationships and development of a novel scoring function for metal-ligand interactions
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We report the discovery of thiabendazole as a potent inhibitor (K 1 = 0.4 μM) of Escherichia coli methionine aminopeptidase (ecMetAP) and the synthesis and pharmacological evaluation of thiabendazole congeners with activity in the upper nanomolar range, Elucidation of the X-ray structure of ecMetAP in complex with thiabendazole and an unrelated inhibitor that was independently described by another group showed that that both compounds bind to an additional CoII ion at the entrance of the active site. This unexpected finding explains the inactivity of the compounds under in vivo conditions. It also allows us to discuss the structure-activity relationships of this series of compounds in a meaningful way, based upon docking runs with an auxiliary metal ion, We describe a new scoring function for the evaluation of metal-mediated inhibitor binding that, unlike the previously used scoring function implemented in the docking program, allows us to distinguish between active and inactive compounds, Finally, conclusions for the structure-based design of in vivo-active inhibitors of ecMetAP are drawn.
- Schiffmann, Rolf,Neugebauer, Alexander,Klein, Christian D.
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p. 511 - 522
(2007/10/03)
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- Practical synthesis of 2-(2-isopropylaminothiazol-4-yl)-7-methoxy-1H- quinolin-4-one: Key intermediate for the synthesis of potent HCV NS3 protease inhibitor BILN 2061
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Herein we describe the development of an efficient, safe and practical process for the synthesis of 7-methoxy-2-(2-amino-4-thiazolyl)quinoline. Our new process allowed for a more convergent approach and eliminates the use of potentially dangerous reagents such as diazomethane used in the previous discovery approach. Georg Thieme Verlag Stuttgart.
- Frutos, Rogelio P.,Haddad, Nizar,Houpis, Ioannis N.,Johnson, Michael,Smith-Keenan, Lana L.,Fuchs, Victor,Yee, Nathan K.,Farina, Vittorio,Faucher, Anne-Marie,Brochu, Christian,Hache, Bruno,Duceppe, Jean-Simon,Beaulieu, Pierre
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p. 2563 - 2567
(2008/02/04)
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- Kinetic study of the Ce(III)-, Mn(II)-, or ferroin-catalyzed Belousov-Zhabotinsky reaction with pyruvic acid
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Ce(III)-, Mn(II)-, or ferroin (Fe(phen)32+)-catalyzed reaction of bromate ion and pyruvic acid (PA) or its dimer exhibits oscillatory behavior. Both the open-chain dimer (parapyruvic acid, γ-methyl-γ-hydroxyl-α-keto-glutaric acid, DP
- Lin, Hsing-Lien,Yu, Yueh-O,Jwo, Jing-Jer
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p. 408 - 418
(2007/10/03)
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- Use of hydroxyphenyl-thiazole-, -thiazoline- and -thiazolidine-carboxylic acids, for influencing the collagen metabolism
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What are disclosed are hydroxyphenyl-thiazole-, -thiazoline- and -thiazolidine-carboxylic acids of the formulae STR1 in which R1 and R3, independently from each other, are hydrogen, methyl, chlorine or bromine, and R1 and R3 may alternatively be nitro, amino or sulfonylamido; R2 is hydrogen, hydroxyl or methyl; R4 is hydrogen or methyl; and R5 is hydrogen, methyl, phenyl or --COOH; and their salts with physiologically acceptable bases, a process for the preparation thereof and their use for influencing the collagen metabolism.
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- Process for the preparation of the potassium salt of phosphoenolpyruvic acid
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The potassium salt of phosphoenolpyruvic acid (PEP-K), used as a phosphorylation agent particularly in enzymatic reactions, is prepared by a process which consists of two steps, namely the treatment of a halopyruvic acid with a trialkyl phosphite and the hydrolysis of the dialkyl phosphate of enolpyruvic acid thus formed in an aqueous medium and in the presence of potassium hydroxide.
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- Oscillatory Chemical Reactions: Part V - Manganese Ion Catalysed Belousov-Zhabotinskii Reaction with Acetylacetone
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The oscillatory reaction in acetylacetone/KBrO3/Mn(+3)/H2SO4 system has been investigated. , and rate of temperature rise (dT/dt) are found to oscillate in phase.No pressure oscillations have been observed.Br(-), Br2, Mn(3+), MnO2, acetic acid and several bromo-derivatives are amongst the reaction products.Both Mn(3+) and BrO3(-) oxidise acetylacetone to acetic acid and pyruvic acid (?).The latter is easily brominated.No CO2 is produced in the reaction.However, in the present case, BrO3(-) is rapidly consumed by acetylacetone producing Br(-) ion which produces Br2 leading to rapid bromination reaction.Thermochemistry of component reactions has been investigated.Initiation time, time period, life time, amplitude and total number of cycles have been determined.Empirical relations between these parameters and concentrations of reactants and temperature have been obtained.
- Rastogi, R. P.,Rastogi, P.
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