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agents halogénés

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https://www.readbyqxmd.com/read/28521262/rhodium-catalyzed-c-h-bond-activation-for-the-synthesis-of-quinonoid-compounds-significant-anti-trypanosoma-cruzi-activities-and-electrochemical-studies-of-functionalized-quinones
#1
Guilherme A M Jardim, Thaissa L Silva, Marilia O F Goulart, Carlos A de Simone, Juliana M C Barbosa, Kelly Salomão, Solange L de Castro, John F Bower, Eufrânio N da Silva Júnior
Thirty four halogen and selenium-containing quinones, synthesized by rhodium-catalyzed C-H bond activation and palladium-catalyzed cross-coupling reactions, were evaluated against bloodstream trypomastigotes of T. cruzi. We have identified fifteen compounds with IC50/24 h values of less than 2 μM. Electrochemical studies on A-ring functionalized naphthoquinones were also performed aiming to correlate redox properties with trypanocidal activity. For instance, (E)-5-styryl-1,4-naphthoquinone 59 and 5,8-diiodo-1,4-naphthoquinone 3, which are around fifty fold more active than the standard drug benznidazole, are potential derivatives for further investigation...
May 4, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28516256/-skin-diseases-associated-with-environmental-factors
#2
REVIEW
Vera Mahler
BACKGROUND: Multiple environmental exposures may derange the regulatory and repair mechanisms of the skin and lead to dermatological disease. OBJECTIVES: Provide an overview of non-allergic skin diseases associated with environmental factors. MATERIALS AND METHODS: Review of current scientific evidence for associations of non-allergic skin diseases with environmental exposures: irritation, chemicals, infection, UV-radiation, temperature. RESULTS: Predisposition (constitution e...
May 17, 2017: Bundesgesundheitsblatt, Gesundheitsforschung, Gesundheitsschutz
https://www.readbyqxmd.com/read/28515440/a-highly-potent-class-of-halogenated-phenazine-antibacterial-and-biofilm-eradicating-agents-accessed-through-a-modular-wohl-aue-synthesis
#3
Hongfen Yang, Yasmeen Abouelhassan, Gena M Burch, Dimitris Kallifidas, Guangtao Huang, Hussain Yousaf, Shouguang Jin, Hendrik Luesch, Robert W Huigens
Unlike individual, free-floating planktonic bacteria, biofilms are surface-attached communities of slow- or non-replicating bacteria encased within a protective extracellular polymeric matrix enabling persistent bacterial populations to tolerate high concentrations of antimicrobials. Our current antibacterial arsenal is composed of growth-inhibiting agents that target rapidly-dividing planktonic bacteria but not metabolically dormant biofilm cells. We report the first modular synthesis of a library of 20 halogenated phenazines (HP), utilizing the Wohl-Aue reaction, that targets both planktonic and biofilm cells...
May 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28500969/oxidation-of-the-antibacterial-agent-norfloxacin-during-sodium-hypochlorite-disinfection-of-marine-culture-water
#4
Yuanyuan Zhang, Chuan Rong, Yanqun Song, Yinghui Wang, Jiying Pei, Xinying Tang, Ruijie Zhang, Kefu Yu
Chlorination disinfection and antibiotic addition are two universal processes of marine culture. The generation of disinfection byproducts (DBPs) is unavoidable. Antibiotic residue not only pollutes water but also acts as a precursor to the production of new DBPs. The fate of antibiotic norfloxacin (NOR) in chlorination disinfection was investigated. It was observed that NOR could be oxidized by disinfection agent sodium hypochlorite, but the oxidation rate varied considerably with the type of disinfected water...
May 7, 2017: Chemosphere
https://www.readbyqxmd.com/read/28499825/induction-of-cytochrome-p450-dependent-mixed-function-oxidase-activities-and-peroxisome-proliferation-by-chloramine-t-in-male-rat-liver
#5
María-Aránzazu Martínez, Irma Ares, Jose-Luís Rodríguez, Marta Martínez, María-Rosa Martínez-Larrañaga, Arturo Anadón
Chloramine-T is an antimicrobial agent recognized for its disinfectant properties widely used in food industry. As an N-chloro-compound, chloramine-T contains electrophilic chlorine and in water it hydrolyses to hypochlorite. Chlorine as hypochlorous acid or hypochlorite is a very reactive chemical which can function as both an oxidant and halogenating agent. Because chloramine-T could be involved in the metabolic activation of drugs, in the present study the effects of chloramine-T on the activities of some drug metabolizing enzymes in rat liver microsomes and peroxisome proliferation were determined in vivo...
May 9, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/28487818/modeling-adsorption-of-brominated-chlorinated-and-mixed-bromo-chloro-dibenzo-p-dioxins-on-c60-fullerene-using-nano-qspr
#6
Piotr Urbaszek, Agnieszka Gajewicz, Celina Sikorska, Maciej Haranczyk, Tomasz Puzyn
Many technological implementations in the field of nanotechnology have involved carbon nanomaterials, including fullerenes such as the buckminsterfullerene, C60. The unprecedented properties of such organic nanomaterials (in particular their large surface area) gained extensive attention for their potential use as organic pollutant sorbents. Sorption interactions can be very hazardous and useful at the same time. This work investigates the influence of halogenation by bromine and/or chlorine in dibenzo-p-dioxins on their sorption ability on the C60 fullerene surface...
2017: Beilstein Journal of Nanotechnology
https://www.readbyqxmd.com/read/28487674/uncovering-potential-applications-of-cyanobacteria-and-algal-metabolites-in-biology-agriculture-and-medicine-current-status-and-future-prospects
#7
REVIEW
Rachana Singh, Parul Parihar, Madhulika Singh, Andrzej Bajguz, Jitendra Kumar, Samiksha Singh, Vijay P Singh, Sheo M Prasad
Cyanobacteria and algae having complex photosynthetic systems can channelize absorbed solar energy into other forms of energy for production of food and metabolites. In addition, they are promising biocatalysts and can be used in the field of "white biotechnology" for enhancing the sustainable production of food, metabolites, and green energy sources such as biodiesel. In this review, an endeavor has been made to uncover the significance of various metabolites like phenolics, phytoene/terpenoids, phytols, sterols, free fatty acids, photoprotective compounds (MAAs, scytonemin, carotenoids, polysaccharides, halogenated compounds, etc...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28480028/a-comparison-of-renal-responses-to-sevoflurane-and-isoflurane-in-patients-undergoing-donor-nephrectomy-a-randomized-controlled-trial
#8
Lady Christine L Ong Sio, Richard Glenn C Dela Cruz, Alexander F Bautista
Sevoflurane and isoflurane are volatile halogenated ether widely used in anesthesia. Both have comparable potency and easy titratability but sevoflurane has lower pungency and results in faster patient recovery. Isoflurane, however, is more affordable. The nephrotoxicity of sevoflurane is undisputed but studies on isoflurane nephrotoxicity are lacking. The objective of this paper is to determine the overall nephrotoxicity profile of sevoflurane and isoflurane in donor nephrectomy patients using the renal function markers - nuclear glomerular filtration rate (GFR), serum creatinine, urine protein-to-creatinine ratio, proteinuria, and glucosuria...
January 2017: Medical Gas Research
https://www.readbyqxmd.com/read/28467047/electrophilic-halogenation-of-closo-1-2-c2b8h10
#9
Mario Bakardjiev, Aleš Růžička, Zdeňka Růžičková, Josef Holub, Oleg L Tok, Bohumil Štíbr
Initial studies on electrophilic halogenation of the dicarbaborane closo-1,2-C2B8H10 (1) have been carried out to reveal that the substitution takes place at B7 and B10 vertexes, which are the most removed from the CH positions. The course of the halogenation is strongly dependent on the nature of the halogenation agent and reaction conditions. Individual reactions led to the isolation of the monosubstituted compounds 1,2-C2B8H9-10-X (2) (where X = F, I) and 1,2-C2B8H9-7-X (3) (where X = Cl, I). Disubstituted carboranes 1,2-C2B8H8-7,10-X2 (4) (where X = Cl, Br, I) were obtained under more forcing conditions...
May 3, 2017: Inorganic Chemistry
https://www.readbyqxmd.com/read/28402644/investigation-of-the-halogenate-hydrogen-peroxide-reactions-using-the-electron-paramagnetic-resonance-spin-trapping-technique
#10
Maja C Pagnacco, Miloš D Mojović, Ana D Popović-Bijelić, Attila K Horváth
The differences in the mechanism of the halogenate reactions with the same oxidizing/reducing agent, such as H2O2 contribute to the better understanding of versatile halogen chemistry. The reaction between iodate, bromate, and chlorate with hydrogen peroxide in acidic medium at 60 °C is investigated by using the electron paramagnetic resonance (EPR) spin trapping technique. Essential differences in the chemistry of iodate, bromate, and chlorate in their reactions with hydrogen peroxide have been evidenced by finding different radicals as governing intermediates...
May 4, 2017: Journal of Physical Chemistry. A
https://www.readbyqxmd.com/read/28384544/design-synthesis-and-structure-activity-relationship-study-of-halogen-containing-2-benzylidene-1-indanone-derivatives-for-inhibition-of-lps-stimulated-ros-production-in-raw-264-7-macrophages
#11
Aarajana Shrestha, Hye Jin Oh, Mi Jin Kim, Nirmala Tilija Pun, Til Bahadur Thapa Magar, Ganesh Bist, Hongseok Choi, Pil-Hoon Park, Eung-Seok Lee
As a continuous effort to discover new potential anti-inflammatory agents, we systematically designed and synthesized sixty-one 2-benzylidene-1-indanone derivatives with structural modification of chalcone, and evaluated their inhibitory activity on LPS-stimulated ROS production in RAW 264.7 macrophages. Systematic structure-activity relationship study revealed that hydroxyl group in C-5, C-6, or C-7 position of indanone moiety, and ortho-, meta-, or para-fluorine, trifluoromethyl, trifluoromethoxy, and bromine functionalities in phenyl ring are important for inhibition of ROS production in LPS-stimulated RAW 264...
March 27, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28380119/synthesis-and-biological-evaluation-of-novel-imidazolidine-derivatives-as-candidates-to-schistosomicidal-agents
#12
Thiago José Matos-Rocha, Maria do Carmo Alves de Lima, Anekécia Lauro da Silva, Jamerson Ferreira de Oliveira, Allana Lemos Andrade Gouveia, Vinícius Barros Ribeiro da Silva, Antônio Sérgio Alves de Almeida, Fábio André Brayner, Pablo Ramon Gualberto Cardoso, Marina da Rocha Pitta-Galdino, Ivan da Rocha Pitta, Moacyr Jesus Barreto de Melo Rêgo, Luiz Carlos Alves, Maira Galdino da Rocha Pitta
Introduction: Schistosomiasis is an infectious parasitic disease caused by trematodes of the genus Schistosoma, which threatens at least 258 million people worldwide and its control is dependent on a single drug, praziquantel. The aim of this study was to evaluate the anti-Schistosoma mansoni activity in vitro of novel imidazolidine derivatives. Material and methods: We synthesized two novel imidazolidine derivatives: (LPSF/PTS10) (Z)-1-(2-chloro-6-fluorobenzyl)-4-(4-dimethylaminobenzylidene)-5-thioxoimidazolidin-2-one and (LPSF/PTS23) (Z)-1-(2-chloro-6-fluoro-benzyl)-5-thioxo-4-(2,4,6-trimethoxy-benzylidene)-imidazolidin-2-one...
April 3, 2017: Revista do Instituto de Medicina Tropical de São Paulo
https://www.readbyqxmd.com/read/28373861/environmental-issues-in-thyroid-diseases
#13
REVIEW
Silvia Martina Ferrari, Poupak Fallahi, Alessandro Antonelli, Salvatore Benvenga
Environmental factors are determinant for the appearance of autoimmune thyroid diseases (AITD) in susceptible subjects. Increased iodine intake, selenium, and vitamin D deficiency, exposure to radiation, from nuclear fallout or due to medical radiation, are environmental factors increasing AITD. Cigarette smoking is associated with Graves' disease and Graves' ophthalmopathy, while it decreases the risk of hypothyroidism and thyroid autoimmunity. Viral infections are important environmental factors in the pathogenesis of AITD, too, particularly human parvovirus B19 (EVB19) and hepatitis C virus...
2017: Frontiers in Endocrinology
https://www.readbyqxmd.com/read/28352158/cardioprotection-with-halogenated-gases-how-does-it-occur
#14
REVIEW
Jose Luis Guerrero-Orriach, Juan Jose Escalona Belmonte, Alicia Ramirez Fernandez, Marta Ramirez Aliaga, Manuel Rubio Navarro, Jose Cruz Mañas
Numerous studies have studied the effect of halogenated agents on the myocardium, highlighting the beneficial cardiac effect of the pharmacological mechanism (preconditioning and postconditioning) when employed before and after ischemia in patients with ischemic heart disease. Anesthetic preconditioning is related to the dose-dependent signal, while the degree of protection is related to the concentration of the administered drug and the duration of the administration itself. Triggers for postconditioning and preconditioning might have numerous pathways in common; mitochondrial protection and a decrease in inflammatory mediators could be the major biochemical elements...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28334702/in-vitro-antibacterial-activity-of-7-substituted-6-fluoroquinolone-and-7-substituted-6-8-difluoroquinolone-derivatives
#15
Socorro Leyva-Ramos, Denisse de Loera, Jaime Cardoso-Ortiz
BACKGROUND: Fluoroquinolones are widely prescribed synthetic antimicrobial agents. Quinolones act by converting their targets, gyrase and topoisomerase IV, into toxic enzymes that fragment the bacterial chromosome; the irreversible DNA damage eventually causes the killing of bacteria. Thorough knowledge of the structure-activity relationship of quinolones is essential for the development of new drugs with improved activity against resistant strains. METHODS: The compounds were screened for their antibacterial activity against 4 representing strains using the Kirby-Bauer disk diffusion method...
2017: Chemotherapy
https://www.readbyqxmd.com/read/28325748/halogenated-ether-alcohol-and-alkane-anesthetics-activate-task-3-tandem-pore-potassium-channels-likely-through-a-common-mechanism
#16
Anita Luethy, James D Boghosian, Rithu Srikantha, Joseph F Cotten
TASK-3 (KCNK9) tandem pore potassium channel function is activated by halogenated anesthetics through binding at a putative anesthetic binding cavity. To understand pharmacological requirements for TASK-3 activation, we studied the concentration-response of TASK-3 to several anesthetics (isoflurane, desflurane, sevoflurane, halothane, α-chloralose, 2,2,2-trichloroethanol(TCE), and chloral hydrate), to ethanol, and to a panel of halogenated methanes and alcohols. We used mutagenesis to probe the anesthetic binding cavity as observed in a TASK-3 homology model...
March 21, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/28306232/synthesis-of-3-5-disubstituted-isoxazoles-containing-privileged-substructures-with-a-diverse-display-of-polar-surface-area
#17
Mingi Kim, Yoon Soo Hwang, Wansang Cho, Seung Bum Park
We designed and synthesized the molecular framework of 3,5-disubstituted isoxazoles containing privileged substructures with various substituents which uniquely display polar surface area in a diverse manner. A library of 3,5-disubstituted isoxazoles were systematically prepared via 1,3-dipolar cycloaddition of alkynes with nitrile oxides prepared by two complementary synthetic routes; method A utilized a halogenating agent with a base and method B utilized a hypervalent iodine reagent. Through the biological evaluation of corresponding isoxazoles via three independent phenotypic assays, the different pattern of biological activities was shown according to the type of privileged substructure and substituent...
March 23, 2017: ACS Combinatorial Science
https://www.readbyqxmd.com/read/28295735/halogen-bonding-interactions-of-polybrominated-diphenyl-ethers-and-thyroid-hormone-derivatives-a-potential-mechanism-for-the-inhibition-of-iodothyronine-deiodinase
#18
Eric S Marsan, Craig A Bayse
Polybrominated diphenyl ethers (PBDEs) increase flame resistance in consumer goods, but these compounds and their hydroxylated derivatives (OH-BDEs) impair normal thyroid function. Halogen bonding (XB) of PBDEs to an active site selenocysteine may prevent iodothyronine deiodinase(Dio)-catalyzed activation/deactivation of thyroid hormone (TH) derivatives. In this study, we compare the strength of the XB interactions of TH derivatives, iodine-based contrast agents and PBDEs/OH-BDEs with a methylselenolate model of the Dio active site using density functional theory calculations...
May 11, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28274352/drug-induced-acne
#19
Jana Kazandjieva, Nikolay Tsankov
A variety of drugs may provoke acne, with drug-induced acne (DIA) often having some specific clinical and histopathologic features. DIA is characterized by a medical history of drug intake, sudden onset, and an unusual age of onset, with a monomorphous eruption of inflammatory papules or papulopustules. The location of the acne lesions is beyond the seborrheic zone. Corticosteroids, anabolic steroids, testosterone, halogens, isoniazid, lithium, and some new anticancer agents are drugs with undoubted causal relationship to acne...
March 2017: Clinics in Dermatology
https://www.readbyqxmd.com/read/28252944/chemical-insights-into-antibacterial-n-halamines
#20
Alideertu Dong, Yan-Jie Wang, Yangyang Gao, Tianyi Gao, Ge Gao
Microbial contamination arising from pathogens poses serious threats to human health and in recent decades has presented an unprecedented challenge to antibacterial research. Of the various antibacterial agents that effectively kill pathogens, halogen-based antibacterial compounds have been successful in eliminating harmful pathogen-associated diseases and are becoming the most popular disinfectants. As a significant subcategory of halogen antibacterial agents, N-halamines have drawn increasing research interest into their chemistry and practical applications...
March 2, 2017: Chemical Reviews
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