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agents halogénés

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https://www.readbyqxmd.com/read/29141200/phosgene-oxime-injury-and-associated-mechanisms-compared-to-vesicating-agents-sulfur-mustard-and-lewisite
#1
Dinesh Giri Goswami, Rajesh Agarwal, Neera Tewari-Singh
Phosgene Oxime (CX, Cl2CNOH), a halogenated oxime, is a potent chemical weapon that causes immediate acute injury and systemic effects. CX, grouped together with vesicating agents, is an urticant or nettle agent with highly volatile, reactive, corrosive, and irritating vapor, and has considerably different chemical properties and toxicity compared to other vesicants. CX is absorbed quickly through clothing with faster cutaneous penetration compared to other vesicating agents causing instantaneous and severe damage...
November 12, 2017: Toxicology Letters
https://www.readbyqxmd.com/read/29121298/human-neural-correlates-of-sevoflurane-induced-unconsciousness
#2
B J A Palanca, M S Avidan, G A Mashour
Sevoflurane, a volatile anaesthetic agent well-tolerated for inhalation induction, provides a useful opportunity to elucidate the processes whereby halogenated ethers disrupt consciousness and cognition. Multiple molecular targets of sevoflurane have been identified, complementing imaging and electrophysiologic markers for the mechanistically obscure progression from wakefulness to unconsciousness. Recent investigations have more precisely detailed scalp EEG activity during this transition, with practical clinical implications...
October 1, 2017: British Journal of Anaesthesia
https://www.readbyqxmd.com/read/29064248/highly-efficient-room-temperature-phosphorescence-from-halogen-bonding-assisted-doped-organic-crystals
#3
Lu Xiao, Yishi Wu, Jianwei Chen, Zhenyi Yu, Yanping Liu, Jiannian Yao, Hongbing Fu
The development of metal-free organic room temperature phosphorescence (RTP) materials has attracted increasing attention because of their applications in sensors, biolabeling (imaging) agents and anticounterfeiting technology, but remains extremely challenging owing to the restricted spin-flip intersystem crossing (ISC) followed by low-yield phosphorescence that cannot compete with nonradiative relaxation processes. Here, we report a facile strategy to realize highly efficient RTP by doping iodo difluoroboron dibenzoylmethane (I-BF2dbm-R) derivatives into a rigid crystalline 4-iodobenzonitrile (Iph-C≡N) matrix...
November 7, 2017: Journal of Physical Chemistry. A
https://www.readbyqxmd.com/read/29055398/dapsone-as-a-potential-treatment-option-for-henoch-sch%C3%A3-nlein-purpura-hsp
#4
Keum Hwa Lee, Jae Hyon Park, Dong Hyun Kim, Jimin Hwang, Goeun Lee, Jae Seok Hyun, Sung Taik Heo, Ji Hoon Choi, Minwoo Kim, Minhye Kim, Seong Il Kim, Michael Eisenhut, Andreas Kronbichler, Jae Il Shin
Henoch-Schönlein Purpura (HSP, IgA vasculitis) is an immunoglobulin A (IgA) mediated disorder characterized by systemic vasculitis with variable presentation, frequently affecting the skin, mucous membrane, joints, kidneys, and rarely lungs and the central nervous system. Interestingly, enhanced production of interleukin-8 (IL-8) levels are found during active disease and increased levels have been reported in supernatants from human umbilical venous endothelial cells after stimulation with sera from patients affected by HSP...
October 2017: Medical Hypotheses
https://www.readbyqxmd.com/read/29039736/a-novel-central-nervous-system-penetrating-protease-inhibitor-overcomes-human-immunodeficiency-virus-1-resistance-with-unprecedented-am-to-pm-potency
#5
Manabu Aoki, Hironori Hayashi, Kalapala Venkateswara Rao, Debananda Das, Nobuyo Higashi-Kuwata, Haydar Bulut, Hiromi Aoki-Ogata, Yuki Takamatsu, Ravikiran S Yedidi, David A Davis, Shin-Ichiro Hattori, Noriko Nishida, Kazuya Hasegawa, Nobutoki Takamune, Prasanth R Nyalapatla, Heather L Osswald, Hirofumi Jono, Hideyuki Saito, Robert Yarchoan, Shogo Misumi, Arun K Ghosh, Hiroaki Mitsuya
Antiretroviral therapy for HIV-1 infection/AIDS has significantly extended the life expectancy of HIV-1-infected individuals and reduced HIV-1 transmission at very high rates. However, certain individuals who initially achieve viral suppression to undetectable levels may eventually suffer treatment failure mainly due to adverse effects and the emergence of drug-resistant HIV-1 variants. Here, we report GRL-142, a novel HIV-1 protease inhibitor containing an unprecedented 6-5-5-ring-fused crown-like tetrahydropyranofuran, which has extremely potent activity against all HIV-1 strains examined with IC50 values of attomolar-to-picomolar concentrations, virtually no effects on cellular growth, extremely high genetic barrier against the emergence of drug-resistant variants, and favorable intracellular and central nervous system penetration...
October 17, 2017: ELife
https://www.readbyqxmd.com/read/29032753/halogenated-agents-and-cardiovascular-surgery-has-mortality-really-decreased
#6
Giovanni Landoni, Juan Carlos Lopez-Delgado, Chiara Sartini, Simona Tamà, Alberto Zangrillo
Halogenated anesthetic agents (desflurane, isoflurane and sevoflurane) may have cardioprotective properties at therapeutic doses against myocardial intraoperative ischemia-reperfusion injury. Cardioprotection mechanisms are related to mitochondrial and anti-apoptotic signaling pathways. Experimental and human studies have proven that their use may reduce morbidity and mortality in the setting of cardiac surgery, including a reduction in myocardial infarct size and mechanical ventilation needs. On the contrary, total intra-venous propofol based anesthesia may be detrimental...
October 10, 2017: Current Vascular Pharmacology
https://www.readbyqxmd.com/read/29032075/synthesis-structures-and-esi-mass-studies-of-silver-i-derivatives-of-imidazolidine-2-thiones-antimicrobial-potential-and-biosafety-evaluation
#7
Jaspreet K Aulakh, Tarlok S Lobana, Henna Sood, Daljit S Arora, Victoria A Smolinski, Courney E Duff, Jerry P Jasinski
The basic objective of this investigation is to explore potential metallo-organic antimicrobial agents based on silver-heterocyclic-2-thiones. In this respect, a series of silver(I) halide complexes with imidazolidine-2-thiones (L-NR, R=H, Me, Et, Pr(n), Bu(n), Ph), namely, mononuclear [AgX(L-NR)(PPh3)2] (X, R: Cl, Bu, 1; Br, Ph, 7); [AgX(L-NR)3] (Br, Bu, 5; Br, Pr(n), 8) and halogen bridged dinuclear [Ag2(μ-X)2(L-NR)2(PPh3)2] (Cl, Bu(n), 2; Cl, Ph, 3; Cl, Pr(n), 4; Br, Ph, 6) have been synthesized and characterized using modern techniques...
October 7, 2017: Journal of Inorganic Biochemistry
https://www.readbyqxmd.com/read/28994673/an-innovative-technique-to-improve-safety-of-volatile-anesthetics-suction-from-the-cardiopulmonary-bypass-circuit
#8
Francesco De Simone, Luigi Cassarà, Salvatore Sardo, Elena Scarparo, Omar Saleh, Caetano Nigro Neto, Alberto Zangrillo, Giovanni Landoni
CONTEXT: Myocardial injury during cardiac surgery on cardiopulmonary bypass (CPB) is a major determinant of morbidity and mortality. Preclinical and clinical evidence of dose- and time-related cardioprotective effects of volatile anesthetic drugs exist and their use during the whole surgery duration could improve perioperative cardiac protection. Even if administering volatile agents during CPB are relatively easy, technical problems, such as waste gas scavenging, may prevent safe and manageable administration of halogenated vapors during CPB...
October 2017: Annals of Cardiac Anaesthesia
https://www.readbyqxmd.com/read/28974823/antioxidant-activity-of-a-halogenated-monoterpene-isolated-from-a-namibian-marine-algal-plocamium-species
#9
Christ W Shapumba, Michael Knott, Petrina Kapewangolo
The antioxidant potential of various marine natural products is well documented. The aim of this study was to evaluate the antioxidant potential of a rare halogenated monoterpene, namely; 1E,3R,4S,5E,7Z-1-bromo-3,4,8-trichloro-7-(dichloromethyl)-3-methylocta-1,5,7-triene (1) for the first time. This compound was isolated from a Namibian red algal Plocamium species. The antioxidant activity of the compound was evaluated using a series of antioxidant assays, namely; 2,2-diphenyl-1-picryl-hydrazyl radical (DPPH), reducing power, nitric oxide (NO) and hydrogen peroxide (H2O2)...
September 2017: Journal of Food Science and Technology
https://www.readbyqxmd.com/read/28953378/discovery-of-a-potent-and-specific-m-tuberculosis-leucyl-trna-synthetase-inhibitor-s-3-aminomethyl-4-chloro-7-2-hydroxyethoxy-benzo-c-1-2-oxaborol-1-3h-ol-gsk656
#10
Xianfeng Li, Vincent Hernandez, Fernando L Rock, Wai Choi, Yvonne S L Mak, Manisha Mohan, Weimin Mao, Yasheen Zhou, Eric E Easom, Jacob J Plattner, Wuxin Zou, Esther Pérez-Herrán, Ilaria Giordano, Alfonso Mendoza-Losana, Carlos Alemparte, Joaquín Rullas, Iñigo Angulo-Barturen, Sabrinia Crouch, Fátima Ortega, David Barros, M R K Alley
There is an urgent need to develop new and safer antitubercular agents that possess a novel mode of action. We synthesized and evaluated a novel series of 3-aminomethyl 4-halogen benzoxaboroles as Mycobacterium tuberculosis (Mtb) leucyl-tRNA synthetase (LeuRS) inhibitors. A number of Mtb LeuRS inhibitors were identified that demonstrated good antitubercular activity with high selectivity over human mitochondrial and cytoplasmic LeuRS. Further evaluation of these Mtb LeuRS inhibitors by in vivo pharmacokinetics (PK) and murine tuberculosis (TB) efficacy models led to the discovery of GSK3036656 (abbreviated as GSK656)...
October 12, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28898054/synthesis-radiolabeling-and-characterization-of-plasma-protein-binding-ligands-potential-tools-for-modulation-of-the-pharmacokinetic-properties-of-radio-pharmaceuticals
#11
Cristina Müller, Renáta Farkas, Francesca Borgna, Raffaella M Schmid, Martina Benešová, Roger Schibli
The development of (radio)pharmaceuticals with favorable pharmacokinetic profiles is crucial for allowing the optimization of the imaging or therapeutic potential and the minimization of undesired side effects. The aim of this study was, therefore, to evaluate and compare three different plasma protein binders (PPB-01, PPB-02, and PPB-03) that are potentially useful in combination with (radio)pharmaceuticals to enhance their half-life in the blood. The entities were functionalized with a 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) chelator via a l-lysine and β-alanine linker moiety using solid-phase peptide chemistry and labeled with (177)Lu (T1/2 = 6...
September 20, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/28875695/bodipy-derivatives-for-photodynamic-therapy-influence-of-configuration-versus-heavy-atom-effect
#12
Jianhua Zou, Zhihui Yin, Kaikai Ding, Qianyun Tang, Jiewei Li, Weili Si, Jinjun Shao, Qi Zhang, Wei Huang, Xiaochen Dong
Heavy atom effect and configuration are important for BODIPY derivatives to generate singlet oxygen ((1)O2) for photodynamic therapy. Herein, a series of BODIPY derivatives with different halogens were synthesized. (1)O2 quantum yields (QYs) and MTT assay confirm that incorporation of more heavy atoms onto dimeric BODIPY cannot effectively enhance the (1)O2 QYs. Rather, the dark toxicity increases. This phenomenon can be attributed to the competition of heavy atom effect and configuration of dimeric BODIPY...
September 27, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28856042/fluorescence-depth-estimation-from-wide-field-optical-imaging-data-for-guiding-brain-tumor-resection-a-multi-inclusion-phantom-study
#13
Dennis Wirth, Kolbein Kolste, Stephen Kanick, David W Roberts, Frédéric Leblond, Keith D Paulsen
Studies have shown that fluorescent agents demarcate tumor from surrounding brain tissue and offer intraoperative guidance during resection. However, visualization of fluorescence signal from tumor below the surgical surface or through the appearance of blood in the surgical field is challenging. We have previously described red light imaging techniques for estimating fluorescent depths in turbid media. In this study, we evaluate these methods over a broader range of fluorophore concentrations, and investigate the ability to resolve multiple fluorescent emissions in the same plane or at different depths along the axis of imaging...
August 1, 2017: Biomedical Optics Express
https://www.readbyqxmd.com/read/28831410/dataset-of-2-2-4-aryloxybenzylidene-hydrazinyl-benzothiazole-derivatives-for-gqsar-of-antitubercular-agents
#14
Amit S Tapkir, Sohan S Chitlange, Ritesh P Bhole
Fragment based Quantitative structure activity relationship (QSAR) analysis on reported 25 2-(2-(4-aryloxybenzylidene) hydrazinyl) benzothiazole dataset as antitubercular agents were carried out. Molecules in the current dataset were fragmented into six fragments (R1, R2, R3, R4, R5, R6).Group based QSAR Models were derived using Multiple linear regression (MLR) analysis and selected on the basis of various statistical parameters. Dataset of benzothiazole reveled importance of presence of halogen atoms on is essential requirement...
October 2017: Data in Brief
https://www.readbyqxmd.com/read/28782957/zwitterionic-salt-catalyzed-site-selective-monobromination-of-arenes
#15
Xiaodong Xiong, Fei Tan, Ying-Yeung Yeung
A zwitterionic-salt-catalyzed electrophilic monobromination of arenes with high regioselectivity has been developed. Under mild reaction conditions, a wide range of monobrominated aromatic compounds can be obtained in excellent yields. The reaction can be operated using an extremely low catalyst loading (0.05 mol %) with the inexpensive brominating agent N-bromosuccinimide. The versatility of this catalytic protocol has been demonstrated by the scale-up reaction with a 0.01 mol % catalyst loading to provide the selectively halogenated compound in quantitative yield...
August 7, 2017: Organic Letters
https://www.readbyqxmd.com/read/28777497/zn-mg-and-li-tmp-bases-for-the-successive-regioselective-metalations-of-the-1-5-naphthyridine-scaffold-tmp-2-2-6-6-tetramethylpiperidyl
#16
Moritz Balkenhohl, Robert Greiner, Ilya S Makarov, Benjamin Heinz, Konstantin Karaghiosoff, Hendrik Zipse, Paul Knochel
A set of successive regioselective metalations and functionalizations of the 1,5-naphthyridine scaffold are described. A combination of Zn-, Mg-, and Li-TMP (TMP=2,2,6,6-tetramethylpiperidyl) bases and the presence or absence of a Lewis acid (BF3 ⋅OEt2 ) allows the introduction of up to three substituents to the 1,5-naphthyridine core. Also, a novel "halogen dance" reaction was discovered upon metalation of an 8-iodo-2,4-trifunctionalized 1,5-naphthyridine allowing a fourth regioselective functionalization...
August 4, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28760586/inactivation-of-microbicidal-active-halogen-compounds-by-sodium-thiosulphate-and-histidine-methionine-for-time-kill-assays
#17
Barbara Böttcher, Bettina Sarg, Herbert H Lindner, Markus Nagl
Rapid inactivation of antimicrobial test agents after exact incubation times with microorganisms is required in time-kill assays. Sodium thiosulphate and a combination of methionine and histidine were compared for neutralisation of active halogen compounds. Test oxidants were mixed with surplus sodium thiosulphate (3%-6%) or histidine/methionine (1% each) in phosphate-buffered saline and incubated for different times, followed by addition of Staphylococcus aureus, Escherichia coli, or Pseudomonas aeruginosa at 1000CFU/ml...
July 29, 2017: Journal of Microbiological Methods
https://www.readbyqxmd.com/read/28757064/synthesis-and-anti-tumor-evaluation-of-panaxadiol-halogen-derivatives
#18
Shengnan Xiao, Shuai Chen, Yuanyuan Sun, Wuxi Zhou, Huri Piao, Yuqing Zhao
In the current work, 13 novel panaxadiol (PD) derivatives were synthesized by reacting with chloroacetyl chloride and bromoacetyl bromide. Their in vitro antitumor activities were evaluated on three human tumor cell lines (HCT-116, BGC-823, SW-480) and three normal cells (human gastric epithelial cell line-GES-1, hair follicle dermal papilla cell line-HHDPC and rat myocardial cell line-H9C2) by MTT assay. Compared with PD, the results demonstrated that compound 1e, 2d, 2e showed significant anti-tumor activity against three tumor cell lines, the IC50 value of compound 2d against HCT-116 was the lowest (3...
September 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28743492/5-bromoindirubin-3-o-oxiran-2-ylmethyl-oxime-a-long-acting-anticancer-agent-and-a-suicide-inhibitor-for-epoxide-hydrolase
#19
Yoshimi Ichimaru, Takeshi Fujii, Hiroaki Saito, Makoto Sano, Taketo Uchiyama, Shinichi Miyairi
Indirubin 3'-oxime (Indox (1b)) suppresses cancer cell growth (IC50: 15μM towards HepG2 cells) and inhibits cell cycle-related kinases such as cyclin-dependent kinases and glycogen synthase kinase-3β. We have previously reported that the conjugation of 1b with oxirane, a protein-reactive component, enhanced the cytotoxic activity of Indox as determined from the IC50 value (1.7μM) of indirubin 3'-(O-oxiran-2-ylmethyl)oxime (Epox/Ind (1c)). Here we prepared Epox/Ind derivatives with one or two halogen atoms or a methoxy group on the aromatic ring(s) of an Indox moiety and studied the structure-activity relationships of the substituent(s)...
September 1, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28730190/comparison-of-halide-receptors-based-on-h-halogen-chalcogen-pnicogen-and-tetrel-bonds
#20
Steve Scheiner
A series of halide receptors are constructed and the geometries and energetics of their binding to F(-), Cl(-), and Br(-) assessed by quantum calculations. The dicationic receptors are based on a pair of imidazolium units, connected via a benzene spacer. The imidazoliums each donate a proton to a halide in a pair of H-bonds. Replacement of the two bonding protons by Br leads to binding via a pair of halogen bonds. Likewise, chalcogen, pnicogen, and tetrel bonds occur when the protons are replaced, respectively, by Se, As, and Ge...
July 21, 2017: Faraday Discussions
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