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Timothy M Shoup et al.
Molecular imaging and biology : MIB : the official publication of the Academy of Molecular Imaging, 17(2), 257-263 (2014-10-03)
Fatty acid amide hydrolase (FAAH), a catabolic enzyme which regulates lipid transmitters in the endocannabinoid system, is an avidly sought therapeutic and positron emission tomography (PET) imaging target for studies involving addiction and neurological disorders. We report the synthesis of
Jane Hubert et al.
Journal of natural products, 78(7), 1609-1617 (2015-06-24)
The aqueous-ethanolic extract of Tephrosia purpurea seeds is currently exploited in the cosmetic industry as a natural ingredient of skin lotions. The aim of this study was to chemically characterize this ingredient by combining centrifugal partition extraction (CPE) as a
Na Guo et al.
Molecules (Basel, Switzerland), 20(5), 9393-9404 (2015-05-27)
In order to improve the antitumor activity and water solubility of 10-hydroxycamptothecin (HCPT), a series of novel HCPT conjugates were designed and synthesized by conjugating polyethylene glycol (PEG) to the 10-hydroxyl group of HCPT via a valine spacer. The in
Barbara Parrino et al.
European journal of medicinal chemistry, 94, 367-377 (2015-03-18)
Three new ring systems, pyrido[2',3':3,4]pyrrolo[1,2-a]quinoxalines, pyrido[3',2':3,4]pyrrolo[1,2-a]quinoxalines and pyrido[2',3':5,6]pyrazino[2,1-a]isoindoles, were synthesized through an aza-substitution on the already active isoindolo-quinoxaline system and in particular in the position 7 or 4 of the isoindole moiety and in position 5 of the quinoxaline portion.
Apurba K Bhattacharjee et al.
European journal of medicinal chemistry, 90, 209-220 (2014-12-03)
Utilizing our previously reported in silico pharmacophore model for reactivation efficacy of oximes, we present here a discovery of twelve new non-oxime reactivators of diisopropylfluorophosphate (DFP)-inhibited acetylcholinesterase (AChE) obtained through virtual screening of an in-house compound database. Rate constant (kr)
Simon J de Veer et al.
The Biochemical journal, 469(2), 243-253 (2015-05-20)
Laskowski inhibitors regulate serine proteases by an intriguing mode of action that involves deceiving the protease into synthesizing a peptide bond. Studies exploring naturally occurring Laskowski inhibitors have uncovered several structural features that convey the inhibitor's resistance to hydrolysis and
Deblina Sarkar et al.
Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy, 153, 397-401 (2015-09-09)
A highly sensitive and selective benzimidazole based colourimetric chemosensor (HL) for the efficient detection of Ni(2+) has been reported. The synthesized chemosensor HL is highly efficient in detecting Ni(2+) over other metal ions that commonly coexist with Ni(2+) in physiological
Jing-Kun Yan et al.
International journal of biological macromolecules, 72, 333-340 (2014-09-07)
In this study, a new non-toxic, biodegradable, biocompatible and water-soluble carboxylic curdlan bearing the dissociable COOH group in 100% purity, which was prepared by 4-acetamido-TEMPO-mediated oxidation, was hydrophobically modified by deoxycholic acid (DOCA) to attain novel amphiphilic curdlan derivatives (CCDs)
Rémi Rosière et al.
International journal of oncology, 47(3), 1131-1142 (2015-07-24)
Besides the numerous advantages of a chemotherapy administered by the inhalation route for lung cancer therapy, dry powder for inhalation (DPI) offers many advantages compared to other techniques and seems to be a technique that is well-adapted to an anticancer
Luís Novo et al.
Molecular pharmaceutics, 12(1), 150-161 (2014-11-11)
The applicability of small interfering RNA (siRNA) in future therapies depends on the availability of safe and efficient carrier systems. Ideally, siRNA delivery requires a system that is stable in the circulation but upon specific uptake into target cells can
C F Massaro et al.
Fitoterapia, 95, 247-257 (2014-04-08)
Propolis of Australian stingless bees (Tetragonula carbonaria, Meliponini) originating from Corymbia torelliana (Myrtaceae) fruit resins was tested for its antimicrobial activities as well as its flavonoid contents. This study aimed at the isolation, structural elucidation and antibacterial testing of flavanones
Fatih Pekdemir et al.
Dalton transactions (Cambridge, England : 2003), 44(1), 158-166 (2014-11-02)
A supramolecule, 6, based on an electron-donor zinc phthalocyanine (ZnPc) and an electron-acceptor perylene diimide (PDI) has been synthesized and characterized by elemental analysis, UV/Vis, IR, (1)H NMR and solid state (13)C CPMAS NMR and also MALDI-TOF and ICP mass
Scott R Pollack et al.
Journal of labelled compounds & radiopharmaceuticals, 58(11-12), 433-441 (2015-09-19)
Omeprazole (Prilosec®) is a selective and irreversible proton pump inhibitor used to treat various medical conditions related to the production of excess stomach acids. It functions by suppressing secretion of those acids. Radiolabeled compounds are commonly employed in the drug
Katalin Devaine-Pressing et al.
Dalton transactions (Cambridge, England : 2003), 44(27), 12365-12375 (2015-03-26)
Magnesium compounds of tetradentate amino-bis(phenolato) ligands, Mg[L1] (1) and Mg[L2] (2) (where [L1] = 2-pyridyl-N,N-bis(2-methylene-4-methoxy-6-tert-butylphenolato), and [L2] = dimethylaminoethylamino-N,N-bis(2-methylene-4-methyl-6-tert-butylphenolato)) were prepared. The proligands, H2[L1] and H2[L2] were reacted with di(n-butyl)magnesium in toluene to give the desired compounds in high yields.
Wei Wang et al.
Journal of agricultural and food chemistry, 63(1), 200-207 (2014-12-18)
Three new phenolic compounds, coretinphenol (1), coretincone (2), and coretinphencone (3), were isolated from the buds of Coreopsis tinctoria Nutt., together with nine known compounds, including butein (4), okanin (5), isoliquiritigenin (6), maritimetin (7), taxifolin (8), isookanin (9), marein (10)
Noorullah Baig et al.
Bioorganic chemistry, 63, 110-115 (2015-10-18)
Six amino acid derived N-glycoconjugates of d-glucose were synthesized, characterized and tested for antibacterial activity against G(+)ve (Bacillus cereus) as well as G(-)ve (Escherichia coli and Klebsiella pneumoniae) bacterial strains. All the tested compounds exhibited moderate to good antibacterial activity
Aditya Kapil Valiveti et al.
Bioorganic & medicinal chemistry, 23(15), 4899-4910 (2015-06-06)
Presently available medications for treatment of organiphosphorus poisoning are not sufficiently effective due to various pharmacological and toxicological reasons. In this regard, herein we report the synthesis of a series of N-thiazolylacetamide monoquaternary pyridinium oximes and its analogs (1a-1b to
Jing-Can Qin et al.
Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy, 152, 352-357 (2015-08-02)
Two Schiff-base fluorescent sensors have been synthesized, which both can act as fluorescent probes for Al(3+), upon addition of Al(3+), they exhibit a large fluorescence enhancement which might be attributed to the formation of 1:1 ligand-Al complexes which inhibit photoinduced
J Aerts et al.
Mediators of inflammation, 2015, 510679-510679 (2015-09-10)
A hydroxypyrone-based matrix metalloproteinase (MMP) inhibitor was synthesized and assayed for its inhibitory capacity towards a panel of ten different MMPs. The compound exhibited selective inhibition towards MMP-12. The effects of inhibition of MMP-12 on endotoxemia and inflammation-induced blood-cerebrospinal fluid
Xiaofei Chen et al.
Macromolecular bioscience, 15(11), 1563-1570 (2015-07-15)
Herein, a novel kind of intelligent nanogels have been designed, which can spatiotemporally control the release of drug (doxorubicin) and photosensitizers (porphyrins) to combine chemo-therapy and photodynamic therapy. Further, the fluorescing properties of porphyrins make it possible to be used
Fen-Fen Zhang et al.
Carbohydrate research, 402, 81-86 (2014-12-17)
The chemical structure studies on an important related substance of voglibose have been carried out using NMR spectroscopy and single crystal X-ray crystallography. For the structure identification study, hydrochloride monohydrate of this compound was isolated and purified. Its molecular structure
Priya P Netalkar et al.
European journal of medicinal chemistry, 79, 47-56 (2014-04-12)
Air and moisture stable coordination compounds of late first row transition metals, viz. Co(II), Ni(II), Cu(II) and Zn(II), with a newly designed ligand, 2-(2-benzo[d]thiazol-2-yl)hydrazono)propan-1-ol (LH), were prepared and successfully characterized using various spectro-analytical techniques. The molecular structures of the ligand
Tsubasa Oyama et al.
Journal of pharmaceutical and biomedical analysis, 116, 71-79 (2015-07-15)
A new pre-column derivatization reagent with a 6-methoxy-4-quinolone (6-MOQ) moiety for amino acid analysis, 2,5-dioxopyrrolidin-1-yl(2-(6-methoxy-4-oxoquinolin-1(4H)-yl)ethyl) carbonate (6-MOQ-EtOCOOSu), was designed and synthesized. 6-MOQ is a thermo/photostable fluorophore with a high proton-affinity site and sensitive determination could be carried out by a
Ilkoo Noh et al.
Biomaterials, 53, 763-774 (2015-04-22)
Multi-drug delivery focuses on different signaling pathways in cancer cells that have synergistic anti-proliferative effects. In this study, we developed multi-prodrug nanocarriers (MPDNCs) consisting of poly (l-lysine)-carboxylate PTX (PLL-PTX) and hyaluronic acid-conjugated GEM (HA-GEM) for CD44-targeted synergistic biliary cancer therapy.
Mostafa M Ghorab et al.
Acta pharmaceutica (Zagreb, Croatia), 64(4), 419-431 (2014-12-23)
A novel series of thiophenes having biologically active sulfonamide 2-11, 3-methylisoxazole 12, 4-methoxybenzo[d] thiazole 13, quinoline 14, 15, benzoylphenylamino 16, and anthracene-9,10-dione 17 moieties were prepared. Structures of the newly synthesized compounds were established by elemental analysis and spectral data.
Feten Najlaoui et al.
International journal of pharmaceutics, 491(1-2), 323-334 (2015-07-03)
Several ferrocenyl analogues of tamoxifen have already showed strong antiproliferative activity in experimental glioma models. Nevertheless, these compounds are very poorly soluble in water and an adapted formulation is needed. In this work, we have tailored and optimized methylated cyclodextrin
Tatsuhiko Someya et al.
Nucleic acids research, 43(14), 6665-6676 (2015-07-02)
Site-specific labeling of long-chain RNAs with desired molecular probes is an imperative technique to facilitate studies of functional RNA molecules. By genetic alphabet expansion using an artificial third base pair, called an unnatural base pair, we present a post-transcriptional modification
Sudipta Chatterjee et al.
Carbohydrate polymers, 123, 432-442 (2015-04-07)
Fish oil-loaded microcapsules were prepared from oil-in-water emulsions using N-stearoyl O-butylglyceryl chitosan as shell material. The emulsions were prepared by both membrane and ultrasonic emulsification processes under variable conditions to examine the effect of the emulsification process and encapsulation conditions
Vitaliy Kapishon et al.
Biomacromolecules, 16(7), 2040-2048 (2015-06-13)
Alginate-based amphiphilic graft copolymers were synthesized by single electron transfer living radical polymerization (SET-LRP), forming stable micelles during polymerization induced self-assembly (PISA). First, alginate macroinitiator was prepared by partial depolymerization of native alginate, solubility modification and attachment of initiator. Depolymerized
Mykhaylo S Frasinyuk et al.
Organic & biomolecular chemistry, 13(4), 1053-1067 (2014-11-22)
The aminomethylation of hydroxylated isoflavones with 2-aminoethanol, 3-amino-1-propanol, 4-amino-1-butanol, and 5-amino-1-pentanol in the presence of excess formaldehyde led principally to 9-(2-hydroalkyl)-9,10-dihydro-4H,8H-chromeno[8,7-e][1,3]-oxazin-4-ones 4 and/or the tautomeric 7-hydroxy-8-(1,3-oxazepan-3-ylmethyl)-4H-chromen-4-ones 5. The ratio of these tautomers was dependent on solvent polarity, electronic effects of
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