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Purine Derivatives (purine + derivative)
Selected AbstractsPurine Derivatives of 1,2-Disubstituted Cyclohexane Analogues of Nucleosides.CHEMINFORM, Issue 4 2004C. Teran Abstract For Abstract see ChemInform Abstract in Full Text. [source] [4 + 2] Cycloaddition Reaction: Synthesis of 7,9-Diaryl-1,3,5-trimethyl-2,4,8-trioxohexahydro-9H-pyrimido [2,1-g]purine Derivatives.CHEMINFORM, Issue 19 2007B. C. Dutta Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source] Synthesis of [14C]-radiolabelled entecavirJOURNAL OF LABELLED COMPOUNDS AND RADIOPHARMACEUTICALS, Issue 9 2005Marc D. Ogan Abstract Radiolabelled [14C]entecavir, (1), was prepared in 12 steps from (1S,2R,3S,5R)-3-(benzyloxy)-2-(benzyloxymethyl)-6-oxa-bicyclo[3.1.0]hexane 2. The chemical yield of [14C]entecavir was 14% from the epoxide 2. Introduction of [14C] radiolabel was achieved by elaboration of 4,5-diaminopyrimidine 8 with triethyl[14C]orthoformate to purine derivative 9. The radiochemical yield of [14C]entecavir from triethyl[14C]orthoformate was 11.3%. Radiochemical purity of [14C]entecavir determined by HPLC was 99.8%. The specific activity of [14C]entecavir was 108 µCi/mg (29.9 mCi/mmol). Copyright © 2005 John Wiley & Sons, Ltd. [source] NMR Quantification of Tautomeric Populations in Biogenic Purine BasesEUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Issue 9 2009Bartl Abstract Purine bases such as purine, adenine, hypoxanthine, and mercaptopurine are known to exist in several tautomeric forms. Characterization of their tautomeric equilibria is important not only for predicting the regioselectivity of their N -alkylation reactions, but also for gaining knowledge of the patterns with which these compounds of significant biological activity form hydrogen bonds with their biological targets. The tautomeric equilibria of purine and some purine derivatives in methanol and N,N -dimethylformamide solutions were investigated by low-temperature 1H and 13C NMR spectroscopy. The N(7)H and N(9)H tautomeric forms were quantified by integrating the individual 1H NMR signals at low temperatures. The Gibbs free energy differences were calculated and the effects of substitution on the N(7)H/N(9)H ratio discussed. A previously published theoretically predicted mechanism of the tautomeric exchange is compared with our measurements in deuteriated solvents. The influence of concentration on the temperature of coalescence indicates that supramolecular clusters play a significant role in this proton transfer process. (© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2009) [source] Synthesis of C-Nucleosidic ATP Mimics as Potential FGFR3 InhibitorsEUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Issue 10 2006Patricia Busca Abstract Receptor tyrosine kinases (RTKs) play an important role in signal transduction pathways, and in particular, FGFR3 is one of the four RTKs related to the fibroblast growth factor family. This paper describes the synthesis of C-nucleosidic ATP mimics, as potential FGFR3 inhibitors, by nucleophilic epoxide ring-opening followed by in situ O -heterocyclization of 1,2:5,6-dianhydro-3,4-di- O -benzyl- D -mannitol or L -iditol. Cesium carbonate [Cs2CO3] was found to be the best catalyst for the reaction of purine derivatives with these bis-epoxides. (© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2006) [source] Effects of citric acid supplementation on rumen fermentation, urinary excretion of purine derivatives and feed digestibility in steers Cong Wang, Qiang Liu, Jie Meng, Wen Zhu Yang, Xiao Min Yang, Dong Chang He, Kuan Hu Dong and Ying Xiang HuangJOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE, Issue 15 2009Article first published online: 3 NOV 200 The original article to which this Erratum refers was published in Journal of the Science of Food and Agriculture, 2009: 89: Pages 2302-2307 [source] Transport of cytokinins mediated by purine transporters of the PUP family expressed in phloem, hydathodes, and pollen of ArabidopsisTHE PLANT JOURNAL, Issue 1 2003Lukas Bürkle Summary Nucleobases and derivatives like cytokinins and caffeine are translocated in the plant vascular system. Transport studies in cultured Arabidopsis cells indicate that adenine and cytokinin are transported by a common H+ -coupled high-affinity purine transport system. Transport properties are similar to that of Arabidopsis purine transporters AtPUP1 and 2. When expressed in yeast, AtPUP1 and 2 mediate energy-dependent high-affinity adenine uptake, whereas AtPUP3 activity was not detectable. Similar to the results from cell cultures, purine permeases (PUP) mediated uptake of adenine can be inhibited by cytokinins, indicating that cytokinins are transport substrates. Direct measurements demonstrate that AtPUP1 is capable of mediating uptake of radiolabeled trans -zeatin. Cytokinin uptake is strongly inhibited by adenine and isopentenyladenine but is poorly inhibited by 6-chloropurine. A number of physiological cytokinins including trans- and cis- zeatin are also efficient competitors for AtPUP2-mediated adenine uptake, suggesting that AtPUP2 is also able to mediate cytokinin transport. Furthermore, AtPUP1 mediates transport of caffeine and ribosylated purine derivatives in yeast. Promoter,reporter gene studies point towards AtPUP1 expression in the epithem of hydathodes and the stigma surface of siliques, suggesting a role in retrieval of cytokinins from xylem sap to prevent loss during guttation. The AtPUP2 promoter drives GUS reporter gene activity in the phloem of Arabidopsis leaves, indicating a role in long-distance transport of adenine and cytokinins. Promoter activity of AtPUP3 was only found in pollen. In summary, three closely related PUPs are differentially expressed in Arabidopsis and at least two PUPs have properties similar to the adenine and cytokinin transport system identified in Arabidopsis cell cultures. [source] Effect of fortifying concentrate supplement with fibrolytic enzymes on nutrient utilization, milk yield and composition in lactating goatsANIMAL SCIENCE JOURNAL, Issue 3 2009Prokasananda BALA ABSTRACT Thirty lactating Beetle-sannen crossbred goats were randomly divided into 3 groups based on first fortnight milk yield, and then adjusted to body weights to study the effect of fibrolytic enzyme supplementation on digestibility and milk production. Goats in the control group (C) were fed 500 g of concentrate supplement (CS) without exogenous fibrolytic enzymes (control; CG) or CS fortified with cellulase and xylanases @ of 4000 and 12500 (EG1) or 8000 and 18 750 IU/kg (EG2), respectively. CS was offered in two equal proportions just after milking at 7 and 17 h. After feeding CS, goats were fed 1200 g of wheat straw as roughage in two equal parts at 08.00 and 18.00 hours. Milk yield was studied for 3½ months. Milking was done by hand. Changes in body weight were also recorded. After a preliminary period of 60 days of feeding, a 7-day digestibility trial was conducted in two intervals with 5 animals from each group at a time. The increase in either wheat straw or NDF intake due to the enzyme mixture was only 3%. There was significant improvement (P < 0.05) in the diet digestibility of DM, OM, CP, NDF, ADF and total carbohydrates (TC) between the control and EG1 and EG2 goats. Improvements were greater (P < 0.05) in the latter group. Microbial protein (MBP) was estimated based on purine derivatives and creatinine excreted in spot urine samples. MBP increased about 10 and 15% in EG1 and EG2, but these values were statistically invalid. Phenomenally milk yield, fat and SNF were significantly (P < 0.001) changed with progression of lactation. On a temporal basis, fortnightly changes in FCM yield of this study could be grouped as 1 month each of first and last and 1½ of middle phase of lactation. Repeated measure analysis showed 180 to 260 mL/day of higher FCM and 16 to 20 g/day of higher SNF yield (P < 0.001) in EG2 than control or even EG1 during 5 to 7th fortnight. However, no significant impact (P > 0.05) was noticed on TF. Feed intake, g/kg FCM yield was also 7% less in EG2 than either CG or EG1. The study concluded that apart from increased digestibility, fortification of CS with cellulase and xylanases enzymes improved FCM yield in the last quarter of lactation in goats, and improved body weights by 5% (P > 0.05). While the digestibility of the diet was higher in EG1 and EG2, the impact on FCM and SNF yield was noticed only on EG2. Our study indicated that CS of lactating goats may be fortified with 8000 and 18 500 IU/kg CS in the last quarter of lactation. [source] The comparative study digestion and metabolism of nitrogen and purine derivatives in male, Thai, Swamp buffalo and Thai, Brahman cattleANIMAL SCIENCE JOURNAL, Issue 2 2009Thongsuk JETANA ABSTRACT Studies on in vivo digestion, rates of passages, metabolism of nitrogen, urinary purine derivative excretion and blood metabolites were carried out in Thai Brahman cattle and Thai swamp buffaloes (16 months old). The animals were fed mixed diets based on pineapple (Ananas comusus) waste silage containing urea-N (NPN) and true protein from a concentrate (TP). The Brahman cattle (310 ± 15 kg) were heavier than the swamp buffaloes (195 ± 9.4 kg) and had higher dry matter (DM), organic matter (OM) and neutral detergent fiber (NDF) intakes when compared on the basis of their metabolic body weight (BW0.75), but these intakes did not differ significantly when the diets of each animal species were compared. The total tract, apparent digestibilities of dry matter (DM) and organic matter (OM) were not significantly different between the animal species when comparing the two types of diets. The NDF digestibility was significantly (P < 0.01) decreased in both animal species when fed the TP diet, but was significantly (P < 0.01) greater in cattle than in swamp buffaloes. The passage rate digesta k1 (P < 0.01) and the passage rate digesta k2 (through the caecum and proximal colon) (P < 0.03) were significantly slower, and the total mean retention time (TMRT) (P < 0.01) was significantly longer in swamp buffaloes when compared to Brahman cattle, but the transit time (TT) showed no difference (P = 0.07) between the animal species or the diets. The N intakes were not different in both animal species and diets, but urine-N was greater (P < 0.05) in Brahman cattle than that in swamp buffaloes. Urine N and digestibility of N were significantly (P < 0.04) higher in animals fed the NPN diet than those fed the TP diet. Urinary purine derivatives (PD) and the creatinine (Cr) excretion of swamp buffaloes were significantly (P < 0.01) lower than those in Brahman cattle. Plasma urea-N (BUN) concentration was significantly (P < 0.01) higher in swamp buffaloes than that in Brahman cattle, but plasma glucose and insulin concentrations were significantly (P < 0.01) higher in Brahman cattle than in swamp buffaloes. The concentrations of non-esterified fatty acids (NEFA) were not significantly (P > 0.05) different in animals fed different diets. The present study demonstrated that Brahman cattle were better in fiber digestibility than swamp buffaloes at utilizing pineapple waste silage with both N sources. [source] | |||||||||||||