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https://www.readbyqxmd.com/read/28646013/doxorubicin-effect-on-myocardial-metabolism-as-a-pre-requisite-for-subsequent-development-of-cardiac-toxicity-a-translational-18-f-fdg-pet-ct-observation
#1
Matteo Bauckneht, Giulia Ferrarazzo, Francesco Fiz, Silvia Morbelli, Matteo Sarocchi, Fabio Pastorino, Alberto Ghidella, Elena Pomposelli, Maurizio Miglino, Pietro Ameri, Laura Emionite, Flavia Ticconi, Eleonora Arboscello, Ambra Buschiazzo, Elena Augusta Massimelli, Salvatore Fiordoro, Anna Borra, Vanessa Cossu, Annalisa Bozzano, Adalberto Ibatici, Mirco Ponzoni, Paolo Spallarossa, Andrea Gallamini, Paolo Bruzzi, Gianmario Sambuceti, Cecilia Marini
The present translational study aimed to verify whether serial (18)F-fluoro-deoxyglucose Positron Emission Tomography/Computed Tomography (FDG-PET/CT), predicts doxorubicin cardiotoxicity. Methods: Fifteen athymic mice were treated with intravenous administration of saline (n = 5), doxorubicin 5 mg/Kg (n = 5) or doxorubicin 7.5 mg/Kg (n = 5) and submitted to dynamic microPET scan to estimate left ventricular glucose consumption (LV-MRGlu) before and after chemotherapy. Thereafter, we retrospectively identified 69 patients successfully treated with Adriamycin, Bleomycin, Vinblastine, and Dacarbazine (ABVD) regimen for Hodgkin's Disease (HD) and submitted to four consecutive FDG-PET/CT scans...
June 23, 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/28643821/non-invasive-approaches-in-the-diagnosis-of-acute-rejection-in-kidney-transplant-recipients-part-i-in-vivo-imaging-methods
#2
REVIEW
Oriane Hanssen, Pauline Erpicum, Pierre Lovinfosse, Paul Meunier, Laurent Weekers, Luaba Tshibanda, Jean-Marie Krzesinski, Roland Hustinx, François Jouret
Kidney transplantation (KTx) represents the best available treatment for patients with end-stage renal disease. Still, full benefits of KTx are undermined by acute rejection (AR). The diagnosis of AR ultimately relies on transplant needle biopsy. However, such an invasive procedure is associated with a significant risk of complications and is limited by sampling error and interobserver variability. In the present review, we summarize the current literature about non-invasive approaches for the diagnosis of AR in kidney transplant recipients (KTRs), including in vivo imaging, gene expression profiling and omics analyses of blood and urine samples...
February 2017: Clinical Kidney Journal
https://www.readbyqxmd.com/read/28643722/endogenous-endophthalmitis-caused-by-cryptococcus-neoformans-var-gattii-mimicking-choroidal-tumor-from-positron-emission-tomography-computed-tomography-to-histopathology
#3
Chun-Ju Lin, Wen-Lu Chen, Jane-Ming Lin, Peng-Tai Tien, Yi-Yu Tsai
A 60-year-old immunocompetent female with pneumonia history about 10 years ago suffered from blurred vision overall survival for 3 weeks. Common cold with headache and unintentional body weight loss was also noted recently. Choroidal detachment simulating choroidal tumor was observed in the temporal quadrant. The 18F-fluoro-2-deoxyglucose (FDG) positron-emission tomography/computed tomography (CT) scan showed focal, mild to moderate FDG uptake in the left lateral orbit, and an enhanced lesion was seen on the recent CT scan...
June 2017: Indian Journal of Ophthalmology
https://www.readbyqxmd.com/read/28639718/catalytic-enantioselective-michael-addition-reactions-of-detrifluoroacetylatively-generated-tertiary-enolates
#4
Yi Zhu, Wenzhong Zhang, Haibo Mei, Jianlin Han, Vadim Anatolievich Soloshonok, Yi Pan
This work describes the first example of Michael addition reactions of detrifluoroacetylatively in situ generated tertiary fluoro-enolates with 1-(1-(phenylsulfonyl)vinylsulfonyl)benzene. Excellent enantioselectivity and chemical yields were achieved with application of catalysts (10 mol %) derived from Cu(OTf)2 and (1S,2S)-1,2-diphenylethane-1,2-diamine. These reactions are shown to be of a considerable degree of structural generality allowing preparation of novel type of biologically interesting molecules containing quaternary C-F stereogenic carbon and featuring five-, six, seven-membered rings as well as heterocyclic 3-fluoro-2,3-dihydrochromen-4-one moiety...
June 22, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28639122/targeting-prostate-specific-membrane-antigen-psma-with-f-18-labeled-compounds-the-influence-of-prosthetic-groups-on-tumor-uptake-and-clearance-profile
#5
Vincent Bouvet, Melinda Wuest, Justin J Bailey, Cody Bergman, Nancy Janzen, John F Valliant, Frank Wuest
PURPOSE: Prostate-specific membrane antigen (PSMA) is an important biomarker expressed in the majority of prostate cancers. The favorable positron emission tomography (PET) imaging profile of the PSMA imaging agent 2-(3-(1-carboxy-5-[(6-[(18)F]fluoro-pyridine-3-carbonyl)-amino]-pentyl)-ureido)-pentane-dioic acid [(18)F]DCFPyL in preclinical prostate cancer models and in prostate cancer patients stimulated the development and validation of other fluorine-containing PSMA inhibitors to further enhance pharmacokinetics and simplify production methods...
June 21, 2017: Molecular Imaging and Biology: MIB: the Official Publication of the Academy of Molecular Imaging
https://www.readbyqxmd.com/read/28638647/crystal-structure-of-3s-4r-4-fluoro-3-4-meth-oxy-phen-yl-1-oxo-2-phenyl-1-2-3-4-tetra-hydro-iso-quinoline-4-carb-oxy-lic-acid
#6
Anna Lehmann, Lisa Lechner, Krzysztof Radacki, Holger Braunschweig, Ulrike Holzgrabe
The title compound, C23H18FNO4, crystallized as a racemate. It exhibits a cis conformation with respect to the F atom and the methine H atom. The piperidine ring has a screw-boat conformation. The meth-oxy-phenyl ring and the phenyl ring are inclined to the mean plane of the iso-quinoline ring system by 89.85 (4) and 46.62 (5)°, respectively, and by 78.15 (5)° to one another. In the crystal, mol-ecules are linked by an O-H⋯O hydrogen bond forming chains propagating along the a-axis direction. The chains are linked by C-H⋯F hydrogen bonds, forming layers lying parallel to the ab plane...
June 1, 2017: Acta Crystallographica. Section E, Crystallographic Communications
https://www.readbyqxmd.com/read/28638049/immunomodulatory-effects-of-nanoparticles-on-skin-allergy
#7
Samreen Jatana, Brian C Palmer, Sarah J Phelan, Lisa A DeLouise
In recent years there has been considerable effort to understand the interaction of nanomaterials with the skin. In this study we use an in vivo mouse model of allergic contact dermatitis to investigate how nanoparticles (NPs) may alter allergic responses in skin. We investigate a variety of NPs that vary in size, charge and composition. Results show that small (<200 nm) negative and neutral charged NPs exhibit an immunosuppressive effect but that positively charged NPs do not. Confocal imaging suggests positively charged NPs may penetrate skin to a lesser extent and thereby are less able interact with and alter the local immune responses...
June 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28636995/experimental-study-on-the-therapeutic-effect-and-underlining-mechanisms-of-positron-in-pancreatic-cancer-cells
#8
Ying Wang, Ming Li, Rao Diao, Brian Tung, Dalong Zhang, Yaming Li
The purpose of this study was to assess the potential therapeutic effect of positrons emitted by 18F-2-Deoxy-2-Fluoro-D-Glucose (18F-FDG) on pancreatic cancer cells and elucidate its underlying mechanisms. Pancreatic cancer cells were incubated with different radioactive concentrations of 18F-FDG and evaluated for anti-cancer properties and underlining mechanisms. In addition, three groups of tumor-bearing mice were treated with different doses of 18F-FDG weekly, the tumor growth rate was calculated, and the mice were imaged by positron emission tomography (PET) with 18F-FDG before and after treatment...
June 5, 2017: Oncotarget
https://www.readbyqxmd.com/read/28627031/the-influence-of-oxygen-atoms-on-conformation-and-%C3%AF-%C3%AF-stacking-of-ladder-type-donor-based-polymers-and-their-photovoltaic-properties
#9
Tong Qin, Yue Zang, Wei-Yun Bai, Kai Yao, Yun-Xiang Xu
A novel ladder-type donor pyran-bridged indacenodithiophene (IDTP) is developed by introducing two oxygen atoms into indacenodithiophene unit. IDTP possesses a twisted backbone and leads to facially asymmetric arrangement of side chains, resulting in enhanced local π-π stacking of according polymer poly[(5,5,11,11-tetrakis(4-octylphenyl)-5,11-dihydrothieno[2',3':5,6]pyrano[3,4-g]thieno[3,2-c]isochromene)-alt-4,7-(5-fluoro-2,1,3-benzothiadiazole)] (PIDTP)-FBT, which shows extended absorption range. Moreover, oxygen atoms render deeper highest occupied molecular orbital (HOMO) levels of poly[indacenodithiophene-alt-4,7-(5-fluoro-2,1,3-benzothiadiazole)] (PIDTP)-FBT compared with PIDT-FBT, therefore bringing a higher open-circuit voltage (Voc )...
June 19, 2017: Macromolecular Rapid Communications
https://www.readbyqxmd.com/read/28626533/synthesis-and-anti-hcv-activity-of-a-novel-2-3-dideoxy-2-%C3%AE-fluoro-2-%C3%AE-c-methyl-guanosine-phosphoramidate-prodrug
#10
Wenquan Yu, Ertong Li, Zhigang Lv, Ke Liu, Xiaohe Guo, Yuan Liu, Junbiao Chang
A novel 2',3'-dideoxy-2'-α-fluoro-2'-β-C-methyl-6-methoxy guanosine (8) and its phosphoramidate prodrug (1) have been designed and synthesized. Their biological activity was evaluated in both cytotoxicity and cell-based HCV replicon assays. Neither compounds exhibited cytotoxicity up to the highest concentration tested (100 μM) in the Huh-7 cell line. The prodrug (1) displayed nanomolar level antiviral activity (EC50 = 0.39-1.1 μM) against the HCV genotype (GT) 1a, 1b, 2a, and 1b S282T replicons.
June 8, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28623878/in-vivo-characterisation-of-a-therapeutically-relevant-self-assembling-18-f-labelled-%C3%AE-sheet-forming-peptide-and-its-hydrogel-using-positron-emission-tomography
#11
O Morris, M A Elsawy, M Fairclough, K J Williams, A McMahon, J Grigg, D Forster, A F Miller, A Saiani, C Prenant
Positron emission tomography (PET) and fluorescence labelling have been used to assess the pharmacokinetics, biodistribution and eventual fate of a hydrogel-forming nonapeptide, FEFKFEFKK (F9) in healthy mice, using (18) F-labelled and fluoresceinisothiocyanate (FITC) - labelled F9 analogues. F9 was site-specifically radiolabelled with 2-[(18) F]fluoro-3-pyridinecarboxaldehyde ([(18) F]FPCA) via oxime bond formation. [(18) F]FPCA-F9 in vivo fate was evaluated both as a solution, following intravenous administration, and as a hydrogel when subcutaneously injected...
June 17, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28621371/does-z-equal-1-or-2-enhanced-powder-nmr-crystallography-verification-of-a-disordered-room-temperature-crystal-structure-of-a-p38-inhibitor-for-chronic-obstructive-pulmonary-disease
#12
Cory M Widdifield, Sten O Nilsson Lill, Anders Broo, Maria Lindkvist, Anna Pettersen, Anna Svensk Ankarberg, Peter Aldred, Staffan Schantz, Lyndon Emsley
The crystal structure of the Form A polymorph of N-cyclopropyl-3-fluoro-4-methyl-5-[3-[[1-[2-[2-(methylamino)ethoxy]phenyl]cyclopropyl]amino]-2-oxo-pyrazin-1-yl]benzamide (i.e., AZD7624), determined using single-crystal X-ray diffraction (scXRD) at 100 K, contains two molecules in the asymmetric unit (Z' = 2) and has regions of local static disorder. This substance has been in phase IIa drug development trials for the treatment of chronic obstructive pulmonary disease, a disease which affects over 300 million people and contributes to nearly 3 million deaths annually...
June 16, 2017: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/28616976/synthesis-and-herbicidal-activity-of-pyrido-2-3-d-pyrimidine-2-4-dione-benzoxazinone-hybrids-as-protoporphyrinogen-oxidase-inhibitors
#13
Da-Wei Wang, Qian Li, Kai Wen, Ismail Ismail, Dan-Dan Liu, Cong-Wei Niu, Xin Wen, Guang-Fu Yang, Zhen Xi
To search for new protoporphyrinogen oxidase (PPO, EC 1.3.3.4) inhibitors with improved bioactivity, a series of novel pyrido[2,3-d]pyrimidine-2,4-dione-benzoxazinone hybrids, 9-13, were designed and synthesized. Several compounds with improved tobacco PPO (mtPPO)-inhibiting and promising herbicidal activities were found. Among them, the most potent compound, 3-(7-fluoro-3-oxo-4-(prop-2-yn-1-yl)-3,4-dihydro-2H-benzo[b][1,4] oxazin-6-yl)-1-methylpyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione, 11q, with a Ki value of 0...
June 26, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28613871/discovery-of-n-4-5-4-fluoro-phenyl-3-methyl-2-methylsulfanyl-3h-imidazol-4-yl-pyridin-2-yl-acetamide-cbs-3595-a-dual-p38%C3%AE-mapk-pde-4-inhibitor-with-activity-against-tnf%C3%AE-related-diseases
#14
Wolfgang Albrecht, Anke Unger, Silke M Bauer, Stefan A Laufer
The anti-inflammatory potential of p38 mitogen-activated protein kinase (MAPK) inhibitors was coincidentally expanded to a dual inhibition of p38α MAPK and phosphodiesterase 4 (PDE4) and the potential benefits arising from the blockage of both inflammation-related enzymes were thoroughly investigated. The most promising compound, CBS-3595 (1), was successively evaluated in in vitro experiments as well as in ex vivo and in vivo preclinical studies after administration of 1 to rodents, dogs and monkeys. The resulting data clearly indicated a potent suppression of tumor necrosis factor alpha (TNFα) release...
June 14, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28613292/chemoselective-ratiometric-imaging-of-protein-s-sulfenylation
#15
Christopher T M B Tom, John E Crellin, Hashim F Motiwala, Matthew B Stone, Dahvid Davda, William Walker, Yu-Hsuan Kuo, Jeannie L Hernandez, Kristin J Labby, Lyanne Gomez-Rodriguez, Paul M Jenkins, Sarah L Veatch, Brent R Martin
Here we report a ratiometric fluorescent probe for chemoselective conjugation to sulfenic acids in living cells. Our approach couples an α-fluoro-substituted dimedone to an aminonaphthalene fluorophore (F-DiNap), which upon sulfenic acid conjugation is locked as the 1,3-diketone, changing the fluorophore excitation. F-DiNap reacts with S-sulfenylated proteins at equivalent rates to current probes, but the α-fluorine substitution blocks side-reactions with biological aldehydes.
June 14, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/28613199/efficacy-of-18-f-2-fluoro-2-deoxy-d-glucose-positron-emission-tomography-computerized-tomography-for-bone-marrow-infiltration-assessment-in-the-initial-staging-of-lymphoma
#16
Ali Ozan Öner, Evrim Sürer Budak, Funda Aydın, Ozan Salim, Orhan Kemal Yücel, Bahar Akkaya, Tayfur Toptaş, Adil Boz, Akın Yıldız, Fırat Güngör, Levent Undar
OBJECTIVE: Currently (18)F-2-fluoro-2-deoxy-D-glucose ((18)F-FDG) positron emission tomography/computerized tomography (PET/CT) is being successfully used for staging and follow-up of Hodgkin's lymphoma (HL) and non-Hodgkin's lymphoma (NHL). Various studies have demonstrated that PET/CT effectively detects bone marrow involvement (BMI) and is concordant with bone marrow biopsy (BMB) findings, thus it is deemed as a complementary method. This study was aimed to evaluate(18)F-FDG-PET/CT efficiency for detection of BMI in HL and NHL...
June 1, 2017: Molecular Imaging and Radionuclide Therapy
https://www.readbyqxmd.com/read/28613196/-18-f-fdg-pet-ct-in-initiation-and-progression-of-inflammation-and-infection
#17
Türkan Ertay, Mine Sencan Eren, Meral Karaman, Gülgün Oktay, Hatice Durak
OBJECTIVE: Detection/localization of infection and inflammation is important for the initiation of correct treatment as well as its maintenance. Nuclear medicine imaging methods play an important role in determining infection and inflammation. (18)F-2'-deoxy-2-fluoro-d-glucose ((18)F-FDG) positron emission tomography/computed tomography (PET/CT) is highly sensitive in such cases when used with tomographic cross-sections. In this study, the development and progression of infection and inflammation were monitored on rats by using (18)F-FDG via PET/CT...
June 1, 2017: Molecular Imaging and Radionuclide Therapy
https://www.readbyqxmd.com/read/28612980/copper-catalyzed-oxidative-dehydrogenative-c-sp3-h-bond-amination-of-cyclo-alkanes-using-nh-free-heterocycles-as-amine-sources
#18
Chang-Sheng Wang, Xiao-Feng Wu, Pierre H Dixneuf, Jean-Francois Soule
A copper-catalyzed oxidative C(sp3)-H/N-H coupling of NH-heterocycles with affordable (cyclo)alkanes was developed. This protocol involved C(sp3)-N bond formation via a radical pathway generated by a homolytic cleavage of di-tert-butyl peroxide and trapping of the radical(s) by copper catalysts. The reaction tolerated a series of functional groups, such as bromo, fluoro, ester, ketone, nitrile, methyl and methoxy. NH-free indoles, pyroles, pyrazoles, indazoles and benzotriazoles have been successfully N-alkylated...
June 14, 2017: ChemSusChem
https://www.readbyqxmd.com/read/28612390/spectral-investigations-on-eu-3-sm-3-doped-and-sm-3-eu-3-co-doped-potassium-fluoro-phosphate-glass-emitting-intense-orange-red-for-lighting-applications
#19
Kapuluri Anil Kumar, Singarapu Babu, Vasanthapalli Reddy Prasad, Samadam Damodaraiah, Yadala Chenchu Ratnakaram
Potassium fluoro-phosphate (KFP) glass singly doped with different concentrations of europium (Eu(3+) ) or samarium (Sm(3+) ) or co-doped (Sm(3+) /Eu(3+) ) was prepared, and their luminescence spectra were investigated. The phase composition of the product was verified by X-ray diffraction analysis. Optical transition properties of Eu(3+) in the studied potassium phosphate glass were evaluated in the framework of the Judd-Ofelt theory. The radiative transition rates (AR ), fluorescence branching ratios (β), stimulated emission cross-sections (σe ) and lifetimes (τexp ) for certain transitions or levels were evaluated...
June 14, 2017: Luminescence: the Journal of Biological and Chemical Luminescence
https://www.readbyqxmd.com/read/28610977/novel-3-fluoro-6-methoxyquinoline-derivatives-as-inhibitors-of-bacterial-dna-gyrase-and-topoisomerase-iv
#20
Mark J Mitton-Fry, Steven J Brickner, Judith C Hamel, Rose Barham, Lori Brennan, Jeffrey M Casavant, Xiaoyuan Ding, Steven Finegan, Joel Hardink, Thuy Hoang, Michael D Huband, Meghan Maloney, Anthony Marfat, Sandra P McCurdy, Dale McLeod, Chakrapani Subramanyam, Michael Plotkin, Usa Reilly, John Schafer, Gregory G Stone, Daniel P Uccello, Todd Wisialowski, Kwansik Yoon, Richard Zaniewski, Christopher Zook
Novel (non-fluoroquinolone) inhibitors of bacterial type II topoisomerases (NBTIs) are an emerging class of antibacterial agents. We report an optimized series of cyclobutylaryl-substituted NBTIs. Compound 14 demonstrated excellent activity both in vitro (S. aureus MIC90=0.125μg/mL) and in vivo (systemic and tissue infections). Enhanced inhibition of Topoisomerase IV correlated with improved activity in S. aureus strains with mutations conferring resistance to NBTIs. Compound 14 also displayed an improved hERG IC50 of 85...
June 3, 2017: Bioorganic & Medicinal Chemistry Letters
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