The effect of thermal oxidation of activated carbon (AC) on adsorption capacity of dibenzothiophene (DBT) was investigated. ACs were treated in air by thermal oxidation at different temperature 473,573 and 673 K and t...
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The effect of thermal oxidation of activated carbon (AC) on adsorption capacity of dibenzothiophene (DBT) was investigated. ACs were treated in air by thermal oxidation at different temperature 473,573 and 673 K and thus modified ACs. AC(473), AC(573) and AC(673) were separately available. The oxygen functional groups on the surfaces of the ACs were determined separately by diffuse reflectance infrared Fourier transform spectroscopy and Boehm titration. The influence of the surface chemistry of the ACs on its adsorption towards DBT was discussed. The results showed that after the thermal oxidation of carbon surfaces, its total basicity decreased, while its total acidity increased. The higher the oxidation temperature was. the more the amounts of surface acidic oxygen-containing groups were, and thus the higher the amounts adsorbed of DBT on corresponding carbon were. For the original AC, AC(473), AC(573) and AC(673), the breakthrough amount of the treat fuel with containing 320 mg Sl(-1) was 35.5, 45, 52.5 and 61 ml fuel g(-1) A(-1), respectively, corresponding to the breakthrough capacity of 11.4, 14.5. 16.8 and 19.5 mg of sulfur per gram of adsorbent (mg S g(-1) A(-1)). The adsorption capacity of the AC(473), AC(573) and AC(673) for DBT increased separately by 27.2%, 47.4% and 70.2% compared to the original AC. (C) 2008 Elsevier B.V. All rights reserved.
SAR around non-peptidic potent bombesin receptor subtype-3 (BRS-3) agonist lead 2 is presented. Attempts to replace the carboxylic acid with heterocyclic isosteres to improve oral bioavailability and brain penetration...
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SAR around non-peptidic potent bombesin receptor subtype-3 (BRS-3) agonist lead 2 is presented. Attempts to replace the carboxylic acid with heterocyclic isosteres to improve oral bioavailability and brain penetration are described. (C) 2010 Elsevier Ltd. All rights reserved.
Ribosome-inactivating proteins (RIPs) represent those proteins that universally depurinate conserved alpha-sarcin loops of large rRNAs. In this study, a 0.6-kb fragment of a 5' flanking region preceding a curcin g...
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Ribosome-inactivating proteins (RIPs) represent those proteins that universally depurinate conserved alpha-sarcin loops of large rRNAs. In this study, a 0.6-kb fragment of a 5' flanking region preceding a curcin gene, encoding a type I RIP curcin, of Jatropha curcas L. endosperm was cloned, and its regulation of expression of the beta-glucuronidase (GUS) reporter gene was investigated in transgenic tobacco. Analysis of GUS activities showed that the 0.6-kb flanking fragment of the curcin gene was sufficient to drive the GUS reporter gene expression in tobacco seed. The activity of this flanking fragment was analyzed at different stages of seed development. Histochemical localization of GUS activity indicated that the promoter was specifically active in the endosperm tissue of the dicotyledonous tobacco embryo. Moreover, this activity was first initiated at the heart-shaped embryonic stage during seed development.
Bombesin receptor subtype 3 (BRS-3) is a G protein coupled receptor whose natural ligand is unknown. We developed potent, selective agonist (Bag-1, Bag-2) and antagonist (Bantag-1) ligands to explore BRS-3 function. B...
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Bombesin receptor subtype 3 (BRS-3) is a G protein coupled receptor whose natural ligand is unknown. We developed potent, selective agonist (Bag-1, Bag-2) and antagonist (Bantag-1) ligands to explore BRS-3 function. BRS-3-binding sites were identified in the hypothalamus, caudal brainstem, and several midbrain nuclei that harbor monoaminergic cell bodies. Antagonist administration increased food intake and body weight, whereas agonists increased metabolic rate and reduced food intake and body weight. Prolonged high levels of receptor occupancy increased weight loss, suggesting a lack of tachyphylaxis. BRS-3 agonist effectiveness was absent in Brs3(-/Y) (BRS-3 null) mice but was maintained in Npy(-/-)Agrp(-/-), Mc4r(-/-), Cnr1(-/-), and Lepr(db/db) mice. In addition, Brs3(-/Y) mice lost weight upon treatment with either a MC4R agonist or a CB1R inverse agonist. These results demonstrate that BRS-3 has a role in energy homeostasis that complements several well-known pathways and that BRS-3 agonists represent a potential approach to the treatment of obesity.
This Letter describes a series of potent and selective BRS-3 agonists containing a biarylethylimidazole pharmacophore. Extensive SAR studies were carried out with different aryl substitutions. This work led to the ide...
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This Letter describes a series of potent and selective BRS-3 agonists containing a biarylethylimidazole pharmacophore. Extensive SAR studies were carried out with different aryl substitutions. This work led to the identification of a compound 2-{2-[4-(pyridin-2-yl) phenyl] ethyl}-5-(2,2-dimethylbutyl)-1H-imidazole 9 with excellent binding affinity (IC(50) = 18 nM, hBRS-3) and functional agonist activity (EC(50) = 47 nM, 99% activation). After oral administration, compound 9 had sufficient exposure in diet induced obese mice to demonstrate efficacy in lowering food intake and body weight via BRS-3 activation. (C) 2010 Elsevier Ltd. All rights reserved.
We report SAR studies on a novel non-peptidic bombesin receptor subtype-3 (BRS-3) agonist lead series derived from high-throughput screening hit RY-337. This effort led to the discovery of compound 22e with significan...
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We report SAR studies on a novel non-peptidic bombesin receptor subtype-3 (BRS-3) agonist lead series derived from high-throughput screening hit RY-337. This effort led to the discovery of compound 22e with significantly improved potency at both rodent and human BRS-3. (C) 2010 Elsevier Ltd. All rights reserved.
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