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  • Articles  (11)
  • Chemistry  (8)
  • Male  (3)
  • 2005-2009  (2)
  • 1995-1999  (4)
  • 1990-1994  (5)
  • Chemistry and Pharmacology  (11)
  • 1
    ISSN: 0899-0042
    Keywords: arylpropionic acid ; ketoprofen ; enantiomer ; stereoselectivity ; Coenzyme A thioester ; hybrid triacylglycerols ; inversion ; adipose tissue ; hepatocytes ; Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: The enantiomeric bioinversion of ketoprofen (KP) enantiomers and their incorporation into triacylglycerols were investigated in the rat (1) in vitro, using liver homogenates, subcellular fractions, and hepatocytes, and (2) in vivo, in different tissue samples after oral administration of the radiolabelled compounds. In liver homogenates or subcellular fractions, the enantiomer (S)-ketoprofen (S-KP) was recovered unchanged, whereas (R)-ketoprofen (R-KP) was partially converted into its Coenzyme A (CoA) thioester and inverted to S-KP. Both processes occurred mainly in the mitochondrial fraction. This supports the mechanism of inversion via stereoselective formation of CoA thioesters of R-KP, already described for other non-steroidal anti-inflammatory drugs. Incorporation into triacylglycerols was detected after incubation with intact hepatocytes in the presence of added glycerol. The process was stereoselective for R-KP vs. S-KP (covalently bound radioactivity 26,742 ± 4,665 dpm/106 cells vs. 6,644 ± 3,179 dpm/106 cells, respectively). However, no incorporation was found in liver samples after oral administration of either R-KP or S-KP. On the contrary, in adipose tissue samples a significant and stereoselective formation of hybrid triacylglycerols was observed: 11,076 ± 2,790 dpm.g-1 for R-KP vs. 660 ± 268 dpm.g-1 for S-KP. The incorporated R/S ratio, higher in adipose tissue (R/S = 17) than in hepatocytes (R/S = 4), indicates that fat may be the main tissue store for the xenobiotic R-KP in rats. © 1996 Wiley-Liss, Inc.
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  • 2
    ISSN: 0899-0042
    Keywords: NSAIDs ; enantioselectivity ; prostaglandin E2 ; thromboxane B2 ; HUVEC ; PMN ; keratinocytes ; P388D1 ; platelets ; Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: The pharmacological activity of rac-ketoprofen and its enantiomers was investigated in vitro using different cellular models. The effect of these compounds on arachidonic acid metabolism was assessed by measuring the inhibition of prostanoid generation under the action of several agonists. Thus, we have evaluated the inhibition of (1) thromboxane B2 synthesis in rabbit platelets and human polymorphonuclear leukocytes (PMNs), (2) prostaglandin E2 synthesis in three cultured cells, namely human umbilical vein endothelial cells (HUVEC), human keratinocytes, and mouse macrophage-like P388D1 cells. The IC50 values found for (+)-(S)-ketoprofen were in the range between 0.1 nM and 0.8 μM, being slightly lower in all models than those found for rac-ketoprofen (0.4 nM-3 μM). On the other hand, (-)-(R)-ketoprofen showed inhibition of cyclooxygenase only at concentrations two or three orders of magnitude higher than those required for the (+)-(S) enantiomer. These results, obtained with cell types of relevance for inflammatory processes and with compounds of high optical purity, demonstrate that the prostanoid biosynthesis inhibition caused by the drug rac-ketoprofen is exclusively due to its dextrorotatory enantiomer. © 1993 Wiley-Liss, Inc.
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  • 3
    Electronic Resource
    Electronic Resource
    New York, NY [u.a.] : Wiley-Blackwell
    Journal of Applied Polymer Science 59 (1996), S. 725-735 
    ISSN: 0021-8995
    Keywords: Chemistry ; Polymer and Materials Science
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology , Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics , Physics
    Notes: Aromatic polyimides were synthesized from 2,2-bis(3-amino-4-hydroxyphenyl)hexafluoropropane (6F-OH diamine) and different aromatic dianhydrides by a one-step hightemperature polycondensation, or by a two-step procedure using either thermal or chemical imidization of poly(amic acids), PAA. The obtained polyimides were compared in terms of their chemical structure, molecular weight, mechanical and thermal properties. The reaction of 6F-OH diamine with different aromatic dianhydrides in amide solvents at room temperature resulted in the formation of PAA with moderate molecular weight (ηinh ≤ 0.7 g/dL). The thermal imidization of these PAAs led to brittle hydroxy polyimides (PI-6F-OH). In contrast, chemical imidization of similar PAAs in acetic anhydride and pyridine brought about flexible self-supporting polyimide films. The FTIR analysis indicated that the latter process was accompanied by an esterification of the OH groups in the diamine moieties, resulting in the formation of the polymers with side acetate groups (PI-6F-Ac). The high molecular weight hydroxy polyimides, suitable for preparation of films with good tensile properties, were synthesized by a one-step high-temperature polycondensation in phenolic solvents. All obtained polyimides were well soluble in common organic solvents. The highest solubility was observed for PI-6F-Ac. It was found by means of FTIR and TGA that the polyimides with the R group (R = OH or acetate) in orto position to the nitrogen atom in the diamine moiety underwent a rearrangement to benzoxazoles above 300°C. The starting temperature and conversion of this rearrangement reaction were controlled by the type of R group. The imide-to-benzoxazole rearrangement shifted to lower temperatures, and higher conversion was encountered for the polyimides with side acetate group, PI-6F-Ac, obtained by chemical imidization. © 1996 John Wiley & Sons, Inc.
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  • 4
    Electronic Resource
    Electronic Resource
    New York, NY : Wiley-Blackwell
    Journal für Praktische Chemie/Chemiker-Zeitung 336 (1994), S. 243-246 
    ISSN: 0941-1216
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: The dye-sensitized singlet molecular oxygen-mediated photo-oxidation of a series of substituted model compounds for phenolic-type pesticides was studied in several solvents in the alkaline range. From a kinetic point of view, the feasibility to regulate the environmental photo-oxidative degradation by means of the incorporation of electron- withdrawing or electron-releasing substituents in the phenolic nucleous was demonstrated.The photo-oxidability varies from relatively high quantum yields values (0.11 in the most favourable cases for 2,6-dimethyl-4-bromophenol in organic solvent) to non-reactivity (for highly deactivated compounds such as 2,4-dinitrophenol).
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  • 5
    ISSN: 0947-6539
    Keywords: alkene complexes ; allyl complexes ; C-H activation ; C-C coupling ; iridium ; Chemistry ; General Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: The bis(ethene) complex [Tp*Ir-(C2H4)2] (1*) (Tp* = tris(3,5-dimethyl-1-pyrazol-1-yl)hydroborato) undergoes thermal rearrangement to the hydrido-allyl complex [Tp*IrH(π3-C3H4Me)] (6*), through the intermediacy of the hydrido-vinyl complex [Tp*IrH(C2H3)(C2H4)] (2*). The overall conversion of 1* into 6* corresponds formally to the dimerisation of ethene by an unprecedented pathway that involves sequential C-H bond activation of a coordinated olefin molecule and C-C bond formation by coupling of the resulting vinyl and ethene moieties. Similar transformations have been observed for monosubstituted olefins like propene and 1-butene, while the internal alkene cis-2-butene experiences allylic activation of an sp3 C-H bond, which provides an alternative route to 6*. The extension of these investigations to the analogous complexes of the unsubstituted tris(pyrazolyl)hydroborato ligand Tp is also reported. Mechanistic studies on the formation of the C-C bond by coupling of the vinyl and the olefin ligands suggest the participation of a vinylidene complex (formed by α-H abstraction from the vinyl group), which then rearranges to an allene species. Evidence for the involvement of these and other key reaction intermediates is provided.
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  • 6
    ISSN: 0030-493X
    Keywords: Chemistry ; Analytical Chemistry and Spectroscopy
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: The mass spectra of eight new substituted 2-(p-R2-phenyl)-indole-3-carboxyaldehydes which have potentially useful pharmacological properties, are presented.
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  • 7
    Electronic Resource
    Electronic Resource
    Weinheim : Wiley-Blackwell
    Zeitschrift für anorganische Chemie 586 (1990), S. 79-86 
    ISSN: 0044-2313
    Keywords: Chemistry ; Inorganic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Synthesis and Structure of Bis(3-diethylamino-5-phenyl-1,2,4-dithiazolium)-tetrachlorocobaltat(II)The title compound 1 was prepared by reaction of Tris(1,1-diethyl-3-benzoyl-thioureato)cobalt(III) with SOCl2 in acetonitrile. 1 has been characterized by IR-spectroscopy and VIS-spectroscopy.The structure of 1 has been determined by an X-ray structure analysis. The compound crystallizes in the monoclin space group C2/c with a = 16.224; b = 11.257; c = 17.697 Å; β = 107,43° and Z = 4. The final R value was R = 0.027 for 2073 observed reflections.The cation of 1 is nearly plane with an extended delocalization of electrons. The CoCl42- anion is tetrahedral with two different long Co—Cl pairs. Interionic contacts S … Cl exists between the structural units of the cations and the anion.
    Notes: Die Darstellung der Titelverbindung 1 erfolgt aus Tris(1,1-diethyl-3-benzoyl-thioureato)-cobalt(III) mit SOCl2 in Acetonitril. 1 wird IR-spektroskopisch und durch VIS-Spektren charakterisiert.Die Struktur von 1 wurde durch Röntgenkristallstrukturanalyse bestimmt. Die Verbindung kristallisiert monoklin in der Raumgruppe C2/c mit den Gitterkonstanten a = 16,224; b = 11,257; c = 17,697 Å, β = 107,43° und Z = 4. Der abschließende R-Wert betrug R = 0,027 für 2073 beobachtete Reflexe.Das Kation von 1 ist nahezu planar und weist eine weitreichende Elektronendelokalisierung auf. Das CoCl42--Anion ist tetraedrisch strukturiert und besitzt zwei unterschiedlich lange Co—Cl-Paare. Zwischen Kation- und Anion-Struktureinheiten bestehen über S und Cl interionische Wechselwirkungen.
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  • 8
    ISSN: 0173-0835
    Keywords: Chemistry ; Biochemistry and Biotechnology
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: The effect of the cationic dye Alcian Blue on the silver staining of bacterial lipopolysaccharide and its polysaccharide and lipid A portions in polyacrylamide gels was investigated. The polysaccharide was only stained when the gel was previously treated with the dye. The polysaccharide moiety was found to be responsible for the lipopolysaccharide staining with silver, whereas the lipid A seemed unimportant. Treatment with Alcian Blue may prove useful to detect hydrophilic components of lipopolysaccharide samples that could no be stained by the usual silver staining procedures.
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  • 9
    Publication Date: 1999-12-03
    Description: Osteoporosis and other diseases of bone loss are a major public health problem. Here it is shown that the statins, drugs widely used for lowering serum cholesterol, also enhance new bone formation in vitro and in rodents. This effect was associated with increased expression of the bone morphogenetic protein-2 (BMP-2) gene in bone cells. Lovastatin and simvastatin increased bone formation when injected subcutaneously over the calvaria of mice and increased cancellous bone volume when orally administered to rats. Thus, in appropriate doses, statins may have therapeutic applications for the treatment of osteoporosis.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Mundy, G -- Garrett, R -- Harris, S -- Chan, J -- Chen, D -- Rossini, G -- Boyce, B -- Zhao, M -- Gutierrez, G -- New York, N.Y. -- Science. 1999 Dec 3;286(5446):1946-9.〈br /〉〈span class="detail_caption"〉Author address: 〈/span〉OsteoScreen, 2040 Babcock Road, San Antonio, TX 78229, USA. mundy@uthscsa.edu〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/10583956" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Bone Density/*drug effects ; Bone Morphogenetic Protein 2 ; Bone Morphogenetic Proteins/biosynthesis/genetics/pharmacology ; Cell Line ; Female ; Fibroblast Growth Factor 1 ; Fibroblast Growth Factor 2/pharmacology ; Humans ; Hydroxymethylglutaryl-CoA Reductase Inhibitors/pharmacology ; Lovastatin/*pharmacology ; Male ; Mice ; Mice, Inbred ICR ; Organ Culture Techniques ; Osteoblasts/*drug effects/metabolism ; Osteoclasts/drug effects ; Osteogenesis/*drug effects ; Osteoporosis/drug therapy ; Ovariectomy ; Promoter Regions, Genetic/drug effects ; Rats ; Recombinant Proteins/pharmacology ; Simvastatin/*pharmacology ; Skull ; Transfection ; *Transforming Growth Factor beta
    Print ISSN: 0036-8075
    Electronic ISSN: 1095-9203
    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
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  • 10
    Publication Date: 2005-08-06
    Description: The brain keenly depends on glucose for energy, and mammalians have redundant systems to control glucose production. An increase in circulating glucose inhibits glucose production in the liver, but this negative feedback is impaired in type 2 diabetes. Here we report that a primary increase in hypothalamic glucose levels lowers blood glucose through inhibition of glucose production in rats. The effect of glucose requires its conversion to lactate followed by stimulation of pyruvate metabolism, which leads to activation of adenosine triphosphate (ATP)-sensitive potassium channels. Thus, interventions designed to enhance the hypothalamic sensing of glucose may improve glucose homeostasis in diabetes.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Lam, Tony K T -- Gutierrez-Juarez, Roger -- Pocai, Alessandro -- Rossetti, Luciano -- AG 21654/AG/NIA NIH HHS/ -- DK 20541/DK/NIDDK NIH HHS/ -- DK 45024/DK/NIDDK NIH HHS/ -- DK 48321/DK/NIDDK NIH HHS/ -- T32-AG023475/AG/NIA NIH HHS/ -- New York, N.Y. -- Science. 2005 Aug 5;309(5736):943-7.〈br /〉〈span class="detail_caption"〉Author address: 〈/span〉Departments of Medicine and Molecular Pharmacology, Diabetes Research Center, Albert Einstein College of Medicine, 1300 Morris Park Avenue, Bronx, NY 10461, USA.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/16081739" target="_blank"〉PubMed〈/a〉
    Keywords: Animals ; Astrocytes/metabolism ; Blood Glucose/*metabolism ; Citric Acid Cycle ; Feedback, Physiological ; Glucose/administration & dosage/*metabolism ; Glucose-6-Phosphatase/metabolism ; Hypothalamus/*metabolism ; Injections, Intraventricular ; Lactic Acid/metabolism ; Liver/*metabolism ; Male ; Neurons/metabolism ; Potassium Channels/metabolism ; Pyruvates/*metabolism ; Rats ; Rats, Sprague-Dawley
    Print ISSN: 0036-8075
    Electronic ISSN: 1095-9203
    Topics: Biology , Chemistry and Pharmacology , Computer Science , Medicine , Natural Sciences in General , Physics
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