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Billah M Cooper N Cuss F Davenport RJ Dyke HJ Egan R Ganguly A Gowers L Hannah DR Haughan AF Kendall HJ Lowe C Minnicozzi M Montana JG Naylor R Oxford J Peake JC Piwinski JJ Runcie KA Sabin V Sharpe A Shih NY Warneck JB 《Bioorganic & medicinal chemistry letters》2002,12(12):1621-1623
The syntheses and pharmacological profiles of some 2-trifluoromethyl-8-methoxyquinoline-5-carboxamides are described. SCH351591 is a potent selective inhibitor of phosphodiesterase type 4 (PDE4). 相似文献
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Buckley G Cooper N Dyke HJ Galleway F Gowers L Gregory JC Hannah DR Haughan AF Hellewell PG Kendall HJ Lowe C Maxey R Montana JG Naylor R Picken CL Runcie KA Sabin V Tuladhar BR Warneck JB 《Bioorganic & medicinal chemistry letters》2000,10(18):2137-2140
The synthesis and pharmacological profile of a novel series of 7-methoxybenzofuran-4-carboxamides is described. Some of these compounds were found to be potent inhibitors of phosphodiesterase type 4 (PDE4). 相似文献
3.
Activation of cell wall-associated peroxidase isoenzymes in pea epicotyls by a xyloglucan-derived nonasaccharide 总被引:4,自引:2,他引:2
Warneck Hildegard Maria; Haug Thomas; Seitz Hanns Ulrich 《Journal of experimental botany》1996,47(12):1897-1904
The cell wall-derived xyloglucan nonasaccharide XXFG was foundto increase the extractable activity of distinct cationic cellwall-associated peroxidase isozyme groups isolated from etiolatedpea epicotyls. Peroxidase activation occurred in the first 10h of incubation with the nonasaccharide in the pea epicotylbioassay. At the same time varying concentrations of XXFG causedgrowth inhibition up to 35%. Neither the increase of peroxidaseactivity nor the growth inhibition was restricted to a certainXXFG concentration. The increase in peroxidase activity wasnot just an oligosaccharide effect in general. The correspondingheptasaccharide XXXG neither inhibited growth nor increasedperoxidase activity. The isozymes extracted from pea epicotylswere additionally separated by cation-exchange chromatographyand submitted to isoelectric focusing. With one exception, allof the ionically-bound, cell wall-associated peroxidases presentin pea epicotyls were cationic or slightly anionic. It is proposedthat the growth inhibition caused by XXFG is at least in partthe result of peroxidasecatalysed cell wall tightening inducedby the nonasaccharide. Key words: XXFG, growth inhibition, cell wall-associated peroxidases, cell wall tightening, pea epicotyls 相似文献
4.
Buckley GM Cooper N Dyke HJ Galleway FP Gowers L Haughan AF Kendall HJ Lowe C Maxey R Montana JG Naylor R Oxford J Peake JC Picken CL Runcie KA Sabin V Sharpe A Warneck JB 《Bioorganic & medicinal chemistry letters》2002,12(12):1613-1615
A series of bicyclic heteroaryl ring systems was considered as a replacement for the 3-cyclopentyloxy-4-methoxyphenyl moiety in rolipram resulting in the discovery of 8-methoxyquinoline-5-carboxamides as potent inhibitors of phosphodiesterase type 4 (PDE4). 相似文献
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Showell GA Barnes MJ Daiss JO Mills JS Montana JG Tacke R Warneck JB 《Bioorganic & medicinal chemistry letters》2006,16(9):2555-2558
Sila-substitution of drugs (the carbon/silicon switch) is a concept that is being successfully used for the development of new chemical entities. The (R)-sila-analogue of the antidepressant venlafaxine is devoid of the serotonin reuptake inhibition observed with the marketed drug, leading to a selective noradrenaline reuptake inhibitor displaying anti-emetic properties. 相似文献
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Shirata NK Espoladore LM Filho AL Pittoli JE di Loreto C Pereira SM Maeda MY Utagawa ML da Silva Aguiar L Roteli-Martins C Martinez EG Syrjänen K 《Analytical and quantitative cytology and histology / the International Academy of Cytology [and] American Society of Cytology》2004,26(5):295-300
OBJECTIVE: To correlate high-risk HPV (hrHPV) detection by Hybrid Capture II (HC2) (Digene, Gaithersburg, Maryland, U.S.A.) with DNA content (ploidy) of cervical biopsies analyzed by a computer-assisted system. STUDY DESIGN: Cervical biopsies from 54 women examined at Leonor Mendes de Barros Hospital, S?o Paulo, as part of the Latin American Screening study during 2002--2003, were tested for hrHPV with HC2. All patients had been referred for colposcopic examination due to an abnormal cervical cytology. The final diagnosis included 30 cervicitis, 14 cervical intraepithelial neoplasia (CIN) 1, 5 CIN 2, 4 CIN 3 and 1 squamous cell carcinoma (SCC). Five-micrometer sections of each biopsy were stained with Feulgen-tionine and evaluated with the CAS 200 System (Becton Dickinson, U.S.A.), using the 3.0 software (version 8.1) of the DNA Quantitative Measurement Program (Becton Dickinson). Ploidy was evaluated from histograms obtained by analyzing atypical nuclei. RESULTS: Of the 30 cervicitis cases, 28 (93.3%) were diploid, and hrHPV was detected in 8 (28.5%) of the cases. Two tetraploid cervicitis lesions were observed, 1 positive and 1 negative for hrHPV. Among the CIN 1 lesions, 8 (57.1%) were diploid and 6 (42.8%) aneuploid. Of the latter, 4 (66.6%) were negative and 2 (33.3%) positive for hrHPV. Of the 5 CIN 2 lesions, 2 were diploid, 2 aneuploid and 1 tetraploid; all were positive for hrHPV. All CIN 3 lesions and the SCC proved to be aneuploid and positive for hrHPV. CONCLUSION: The data suggest that the majority of cervicitis and CIN 1 lesions are diploid and negativef or hrHPV. This is in sharp contrast to high grade CIN 2-3 lesions, all of which were positive for hrHPV in this study and also aneuploid, consistent with their progressive potential. 相似文献
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Buckley GM Cooper N Davenport RJ Dyke HJ Galleway FP Gowers L Haughan AF Kendall HJ Lowe C Montana JG Oxford J Peake JC Picken CL Richard MD Sabin V Sharpe A Warneck JB 《Bioorganic & medicinal chemistry letters》2002,12(3):509-512
The synthesis and pharmacological profile of a novel series of 7-methoxy-furo[2,3-c]pyridine-4-carboxamides is described. Some of these compounds were found to be potent inhibitors of phosphodiesterase type 4 (PDE4). 相似文献
8.
Barnes MJ Conroy R Miller DJ Mills JS Montana JG Pooni PK Showell GA Walsh LM Warneck JB 《Bioorganic & medicinal chemistry letters》2007,17(2):354-357
The synthesis, physicochemical properties and pharmacological profiles of two novel silicon-containing p38 MAP kinase inhibitors are described. 相似文献
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When [glucitol-3H]XXFGol (a NaB3H4-reduced xyloglucan nonasaccharide) was applied to excised shoots of pea (Pisum sativum L. cv. Progress) at the base of the epicotyl, it inhibited growth in the elongation zone, 4–5 cm distal. Experiments were
conducted to discover whether such 3H-oligosaccharides are translocated intact over this distance, or whether an intercellular second messenger would have to
be postulated. After 24 h, 3H from [glucitol-3H]XXFGol and [glucitol-3H]XXXGol showed U-shaped distributions, with most 3H at the base and apex of the stem. Radioactivity from [fucosyl-3H]XXFG and [xylosyl-3H]XXFG also moved acropetally, but did not concentrate at the apex, possibly owing to removal from the transpiration stream
of fucose and xylose formed by partial hydrolysis of XXFG en route. When 10−7 M [glucitol-3H]XXFGol was supplied, about 14 fmol · seedling–1 of apparently intact [3H]XXFGol was extractable from the elongation zone after 24 h. Larger amounts of degradation products were extractable (including
free [3H]glucitol) and some wall-bound 3H-hemicellulose was present (presumably formed by the oligosaccharides acting as acceptor substrates for transglycosylation).
We conclude that biologically active oligosaccharides of xyloglucan can move through the stem acropetally and that they are
maintained at low steady-state concentrations by both hydrolysis and transglycosylation.
Received: 1 April 1997 / Accepted: 28 May 1997 相似文献
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Billah M Buckley GM Cooper N Dyke HJ Egan R Ganguly A Gowers L Haughan AF Kendall HJ Lowe C Minnicozzi M Montana JG Oxford J Peake JC Picken CL Piwinski JJ Naylor R Sabin V Shih NY Warneck JB 《Bioorganic & medicinal chemistry letters》2002,12(12):1617-1619
The synthesis and pharmacological profile of a novel series of 2-substituted 8-methoxyquinolines is described. The 2-trifluoromethyl compound was found to be a potent inhibitor of phosphodiesterase type 4 (PDE4). 相似文献
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