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https://www.readbyqxmd.com/read/29334151/fused-tris-thienothiophene-based-electron-acceptor-with-strong-near-infrared-absorption-for-high-performance-as-cast-solar-cells
#1
Tengfei Li, Shuixing Dai, Zhifan Ke, Langxuan Yang, Jiayu Wang, Cenqi Yan, Wei Ma, Xiaowei Zhan
A fused tris(thienothiophene) (3TT) building block is designed and synthesized with strong electron-donating and molecular packing properties, where three thienothiophene units are condensed with two cyclopentadienyl rings. Based on 3TT, a fused octacylic electron acceptor (FOIC) is designed and synthesized, using strong electron-withdrawing 2-(5/6-fluoro-3-oxo-2,3-dihydro-1H-inden-1-ylidene)-malononitrile as end groups. FOIC exhibits absorption in 600-950 nm region peaked at 836 nm with extinction coefficient of up to 2 × 105 m-1 cm-1 , low bandgap of 1...
January 15, 2018: Advanced Materials
https://www.readbyqxmd.com/read/29332593/facile-synthesis-crystal-structure-dft-calculation-and-biological-activities-of-4-2-fluorophenyl-3-3-methoxybenzyl-1h-1-2-4-triazol-5-4h-one-5
#2
Muhammad Saleem, Muhammad Rafiq, Yeon Ki Jeong, Dae Won Cho, Chong-Hyeak Kim, Sung-Yum Seo, Chang-Shik Choi, Seong-Karp Hong, Ki-Hwan Lee
BACKGROUND: In the past few decades, the design, synthesis and characterization of novel heterocyclic compounds with auspicious biological profile received the considerable attention of scientific community. Among them, the small and simple organic molecular backbone like triazole moiety have broad spectrum of applications in the medicinal as well as diagnostic areas. OBJECTIVE: The objective of present study was the synthesis, characterization and exploration of biological profile of 4-(2-fluorophenyl)-3-(3-methoxybenzyl)-1H-1,2,4-triazol-5(4H)-one (5)...
January 12, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29330751/prospective-trial-evaluating-the-sensitivity-and-specificity-of-3-4-dihydroxy-6-18f-fluoro-l-phenylalanine-18f-dopa-pet-and-mri-in-patients-with-recurrent-gliomas
#3
Ryan S Youland, Deanna H Pafundi, Debra H Brinkmann, Val J Lowe, Jonathan M Morris, Bradley J Kemp, Christopher H Hunt, Caterina Giannini, Ian F Parney, Nadia N Laack
Treatment-related changes can be difficult to differentiate from progressive glioma using MRI with contrast (CE). The purpose of this study is to compare the sensitivity and specificity of 18F-DOPA-PET and MRI in patients with recurrent glioma. Thirteen patients with MRI findings suspicious for recurrent glioma were prospectively enrolled and underwent 18F-DOPA-PET and MRI for neurosurgical planning. Stereotactic biopsies were obtained from regions of concordant and discordant PET and MRI CE, all within regions of T2/FLAIR signal hyperintensity...
January 13, 2018: Journal of Neuro-oncology
https://www.readbyqxmd.com/read/29329908/anatomical-evidence-for-lateral-hypothalamic-innervation-of-the-pontine-a7-catecholamine-cell-group-in-rat
#4
Janean E Holden, Monica A Wagner, Brady L Reeves
Substantial behavioral evidence exists to support the idea that the lateral hypothalamus (LH) makes axonal connection with spinally-projecting noradrenergic neurons of the A7 catecholamine cell group in the pons. Through this putative projection, the LH modulates nociception via α1- and α2-adrenoceptors in the dorsal horn. We used double-label immunocytochemistry to demonstrate that axons from the LH labeled with the anterograde tracer biotinylated dextran amine (BDA) appose tyrosine hydroxylase-immunoreactive (TH-ir) neuron profiles in the A7 area...
January 9, 2018: Neuroscience Letters
https://www.readbyqxmd.com/read/29327019/using-a-novel-rigid-fluoride-polymer-to-control-the-interfacial-thickness-of-graphene-and-tailor-the-dielectric-behavior-of-poly-vinylidene-fluoride-trifluoroethylene-chlorotrifluoroethylene-nanocomposites
#5
Xianghui Han, Sheng Chen, Xuguang Lv, Hang Luo, Dou Zhang, Chris R Bowen
Polymer nanocomposites based on conductive fillers for high performance dielectrics have attracted increasing attention in recent years. However, a number of physical issues are unclear, such as the effect of interfacial thickness on the dielectric properties of the polymer nanocomposites, which limits the enhancement of permittivity. In this research, two core-shell structured reduced graphene oxide (rGO)@rigid-fluoro-polymer conducting fillers with different shell thicknesses are prepared using a surface-initiated reversible-addition-fragmentation chain transfer polymerization method, which are denoted as rGO@PTFMS-1 with a thin shell and rGO@PTFMS-2 with a thick shell...
January 12, 2018: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/29325553/sitagliptin-improved-glucose-assimilation-in-detriment-of-fatty-acid-utilization-in-experimental-type-ii-diabetes-role-of-glp-1-isoforms-in-glut4-receptor-trafficking
#6
E Ramírez, B Picatoste, A González-Bris, M Oteo, F Cruz, A Caro-Vadillo, J Egido, J Tuñón, M A Morcillo, Ó Lorenzo
BACKGROUND: The distribution of glucose and fatty-acid transporters in the heart is crucial for energy consecution and myocardial function. In this sense, the glucagon-like peptide-1 (GLP-1) enhancer, sitagliptin, improves glucose homeostasis but it could also trigger direct cardioprotective actions, including regulation of energy substrate utilization. METHODS: Type-II diabetic GK (Goto-Kakizaki), sitagliptin-treated GK (10 mg/kg/day) and wistar rats (n = 10, each) underwent echocardiographic evaluation, and positron emission tomography scanning for [18F]-2-fluoro-2-deoxy-D-glucose (18FDG)...
January 11, 2018: Cardiovascular Diabetology
https://www.readbyqxmd.com/read/29325107/2-o-2-methoxyethyl-nucleosides-are-not-phosphorylated-or-incorporated-into-the-genome-of-human-lymphoblastoid-tk6-cells
#7
Amer F Saleh, Martin Bachman, Catherine C Priestley, Nigel J Gooderham, Patrik Andersson, Scott P Henry, Nick Edmunds, Mick D Fellows
Nucleoside analogues with 2'-modified sugar moieties are often used to improve the RNA target affinity and nuclease resistance of therapeutic oligonucleotides in preclinical and clinical development. Despite their enhanced nuclease resistance, oligonucleotides could slowly degrade releasing nucleoside analogues that have the potential to become phosphorylated and incorporated into cellular DNA and RNA. For the first time, the phosphorylation and DNA and RNA incorporation of 2'-O-(2-methoxyethyl) (2'-O-MOE) nucleoside analogues have been investigated...
January 9, 2018: Toxicological Sciences: An Official Journal of the Society of Toxicology
https://www.readbyqxmd.com/read/29322833/primary-genitourinary-lymphoma-on-fdg-pet
#8
Nikita Naik, Michael Lin, Peter Lin
Primary extra nodal lymphomatous involvement of the genitourinary tract is rare and secondary extra-nodal involvement in disseminated disease occurs more frequently. Imaging of metabolic activity with 2-[fluorine-18] fluoro-2-deoxy-d-glucose (FDG) used in positron emission tomography (PET) facilitates the identification of these extra-nodal sites of disease, particularly in the absence of structural lesions on conventional imaging modalities. Primary extra-nodal lymphoma affecting the genitourinary system is often caused by high-grade Non-Hodgkin's Lymphoma (NHL) with the most common subtype being Diffuse Large B-Cell Lymphoma (DLBCL)...
January 11, 2018: British Journal of Radiology
https://www.readbyqxmd.com/read/29321549/probing-the-molecular-basis-of-herg-drug-block-with-unnatural-amino-acids
#9
Logan C Macdonald, Robin Y Kim, Harley T Kurata, David Fedida
Repolarization of the cardiac action potential is primarily mediated by two voltage-dependent potassium currents: I Kr and I Ks . The voltage-gated potassium channel that gives rise to I Kr, Kv11.1 (hERG), is uniquely susceptible to high-affinity block by a wide range of drug classes. Pore residues Tyr652 and Phe656 are critical to potent drug interaction with hERG. It is considered that the molecular basis of this broad-spectrum drug block phenomenon occurs through interactions specific to the aromatic nature of the side chains at Tyr652 and Phe656...
January 10, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29321384/discovery-of-a-novel-fluoroquinolone-antibiotic-candidate-wfq-228-with-potent-antimicrobial-activity-and-the-potential-to-overcome-major-drug-resistance
#10
Tatsuya Hirano, Tomohiko Kinoshita, Daichi Kazamori, Satoshi Inoue, Kouji Nishimura, Asuka Sakurai, Kensuke Ohishi, Yasuhiro Kuramoto, Hirotaka Amano, Akira Yazaki
WFQ-101 with a unique N-1 substituent, 5-amino-4-fluoro-2-(hydroxymethyl)phenyl group, was selected as a lead compound through combination screening based on antimicrobial activity and the efflux index against quinolone-resistant (QR) Pseudomonas aeruginosa (P. aeruginosa). Through structural optimization, we identified WFQ-228 as a novel fluoroquinolone antibiotic candidate. WFQ-228 had potent and superior activity in comparison to levofloxacin (LVX) and ciprofloxacin (CIP) against clinical isolates of P. aeruginosa, Escherichia coli and Acinetobacter baumannii, including QR strains...
January 11, 2018: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/29319802/functional-analysis-of-arginine-decarboxylase-gene-spea-of-bacteroides-dorei-by-markerless-gene-deletion
#11
Mikiyasu Sakanaka, Yuta Sugiyama, Misaki Nara, Aya Kitakata, Shin Kurihara
Polyamine concentrations in the intestine are regulated by their biosynthesis by hundreds of gut microbial species and these polyamines are involved in host health and disease. However, polyamine biosynthesis has not been sufficiently analyzed in major members of the human gut microbiota, possibly owing to a lack of gene manipulation systems. In this study, we successfully performed markerless gene deletion in Bacteroides dorei, one of the major members of the human gut microbiota. The combination of a thymidine kinase gene (tdk) deletion mutant and a counter-selection marker tdk, which has been applied in other Bacteroides species, was used for the markerless gene deletion...
January 8, 2018: FEMS Microbiology Letters
https://www.readbyqxmd.com/read/29317164/progress-in-antischistosomal-n-n-diaryl-urea-sar
#12
Jianbo Wu, Chunkai Wang, Derek Leas, Mireille Vargas, Karen L White, David M Shackleford, Gong Chen, Austin G Sanford, Ryan M Hemsley, Paul H Davis, Yuxiang Dong, Susan A Charman, Jennifer Keiser, Jonathan L Vennerstrom
N,N'-Diaryl ureas have recently emerged as a new antischistosomal chemotype. We now describe physicochemical profiling, in vitro ADME, plasma exposure, and ex vivo and in vivo activities against Schistosoma mansoni for twenty new N,N'-diaryl ureas designed primarily to increase aqueous solubility, but also to maximize structural diversity. Replacement of one of the 4-fluoro-3-trifluoromethylphenyl substructures of lead N,N'-diaryl urea 1 with azaheterocycles and benzoic acids, benzamides, or benzonitriles decreased lipophilicity, and in most cases, increased aqueous solubility...
December 29, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29317048/imaging-skeletal-muscle-volume-density-and-fdg-uptake-before-and-after-induction-therapy-for-non-small-cell-lung-cancer
#13
M D Goncalves, S Taylor, D F Halpenny, E Schwitzer, S Gandelman, J Jackson, A Lukose, A J Plodkowski, K S Tan, M Dunphy, L W Jones, R J Downey
AIM: To assess whether changes in body composition could be assessed serially using conventional thoracic computed tomography (CT) and positron-emission tomography (PET)/CT imaging in patients receiving induction chemotherapy for non-small cell lung cancer (NSCLC). MATERIALS AND METHODS: CT-based skeletal muscle volume and density were measured retrospectively from thoracic and lumbar segment CT images from 88 patients with newly diagnosed and untreated NSCLC before and after induction chemotherapy...
January 6, 2018: Clinical Radiology
https://www.readbyqxmd.com/read/29316696/protective-effects-of-protocatechuic-acid-on-seizure-induced-neuronal-death
#14
Song Hee Lee, Bo Young Choi, A Ra Kho, Jeong Hyun Jeong, Dae Ki Hong, Sang Hwon Lee, Sang Yup Lee, Min Woo Lee, Hong Ki Song, Hui Chul Choi, Sang Won Suh
Protocatechuic acid (PCA) is a type of phenolic acid found in green tea and has been shown to have potent antioxidant and anti-inflammatory properties. However, the effect of PCA on pilocarpine seizure-induced neuronal death in the hippocampus has not been evaluated. In the present study, we investigated the potential therapeutic effects of PCA on seizure-induced brain injury. Epileptic seizure was induced by intraperitoneal (i.p.) injection of pilocarpine (25 mg/kg) in adult male rats, and PCA (30 mg/kg) was injected into the intraperitoneal space for three consecutive days after the seizure...
January 8, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29315577/bidirectional-variation-in-glutamate-efflux-in-the-medial-prefrontal-cortex-induced-by-selective-positive-and-negative-allosteric-mglur5-modulators
#15
Sarah N Isherwood, Trevor W Robbins, Jeffrey W Dalley, Anton Pekcec
Dysregulation of prefrontal cortical glutamatergic signalling via NMDA receptor hypofunction has been implicated in cognitive dysfunction and impaired inhibitory control in such neuropsychiatric disorders as schizophrenia, attention deficit hyperactivity disorder and drug addiction. Although NMDA receptors functionally interact with metabotropic glutamate receptor 5 (mGluR5), the consequence of this interaction for glutamate release in the prefrontal cortex (PFC) is unknown. We therefore investigated the effects of positive and negative allosteric mGluR5 modulation on changes in extracellular glutamate efflux in the medial PFC (mPFC) induced by systemic administration of the non-competitive NMDA receptor antagonist dizocilpine (or MK801) in rats...
January 6, 2018: Journal of Neurochemistry
https://www.readbyqxmd.com/read/29314161/a-novel-synthesis-of-6-18-f-fluoromaltotriose-as-a-pet-tracer-for-imaging-bacterial-infection
#16
Mohammad Namavari, Gayatri Gowrishankar, Ananth Srinivasan, Sanjiv S Gambhir
The aim of this study was to develop a positron emission tomography (PET) tracer to visualize and monitor therapeutic response to bacterial infections. In our continued efforts to find maltose based PET tracers that can image bacterial infections, we have designed and prepared 6''-[18 F]fluoromaltotriose as a second generation PET imaging tracer targeting the maltodextrin transporter of bacteria. We have developed methods to synthesize 6''-deoxy-6''-[18 F]fluoro-α-D-glucopyranosyl-(1-4)-O-α-D-glucopyranosyl-(1-4)-O-D-glucopyranose (6''-[18 F]-fluoromaltotriose) as a bacterial infection PET imaging agent...
January 4, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/29313686/organocatalytic-stereoselective-synthesis-of-fluorinated-3-3-linked-bisoxindoles
#17
Max Moskowitz, Kaluvu Balaraman, Christian Wolf
A highly diastereoselective organocatalytic method that produces 3-fluoro-3'-hydroxy-3,3'-bisoxindoles and the corresponding 3-fluoro-3'-amino derivatives having two adjacent chirality centers from fluorooxindoles and isatins in high yields is described. The reaction occurs in protic solvents at room temperature, it can be upscaled without compromising yield and stereoselectivity, and chromatographic product purification is not required.
January 9, 2018: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/29313599/neurodegeneration-in-zebrafish-embryos-and-adults-after-cadmium-exposure
#18
Antonio Monaco, Teresa Capriello, Maria C Grimaldi, Valentina Schiano, Ida Ferrandino
Cadmium is a biologically non-essential metal. It is also toxic to many organs including the brain. The aim of this study was to analyse the neurodegenerative effects of this metal in embryos and adults of zebrafish exposed to sub-lethal concentrations of cadmium. The study was performed by cytochemical stainings. Six hours after fertilisation (hpf) zebrafish embryos were treated for 24 hours with 9 μM of cadmium and subsequently stained with Acridine orange in whole mount to detect apoptosis in the brain...
October 19, 2017: European Journal of Histochemistry: EJH
https://www.readbyqxmd.com/read/29313047/photoacidity-as-a-tool-to-rationalize-excited-state-intramolecular-proton-transfer-reactivity-in-flavonols
#19
Luís Gustavo Teixeira Alves Duarte, José Carlos Germino, Cláudia de Ávila Braga, Cristina Aparecida Barboza, Teresa Dib Zambon Atvars, Fabiano da Silveira Santos, Fabiano Severo Rodembusch
This work presents the determination of acidic strengths at the electronic ground and excited states (pKa and ) of three flavonol derivatives using electronic absorption and fluorescence emission spectroscopy. The differences of the pKa and values were successfully correlated with the molecular structures according to the substitution pattern at the flavonol structure (hydrogen, diethylamino or fluoro moieties). In order to obtain more information about the observed photoacidity of these superacids, geometry optimizations and excitation energy calculations were performed at the CAM-B3LYP/6-311++G(d,p) level for their neutral, protonated and deprotonated species...
January 9, 2018: Photochemical & Photobiological Sciences
https://www.readbyqxmd.com/read/29311752/computational-design-and-synthesis-of-novel-fluoro-analogs-of-combretastatins-a-4-and-a-1
#20
Yao Zong, Christie Shea, Katherine Maffucci, Iwao Ojima
Combretastatin A-1 (CA-1) and combretastatin A-4 (CA-4) isolated from the African bush willow Combretum caffrum are highly potent tubulin polymerization inhibitors, possessing strong antitumor activities because of their vascular disrupting properties. Extensive SAR studies have been done for CA-4 analogs. Because of poor solubility, water-soluble prodrugs of CA-4 and CA-1 have been developed, which are currently in human clinical trials. Fluorine plays an important role in the current drug discovery and development due to its unique properties...
November 2017: Journal of Fluorine Chemistry
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