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agents halogénés

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https://www.readbyqxmd.com/read/28334702/in-vitro-antibacterial-activity-of-7-substituted-6-fluoroquinolone-and-7-substituted-6-8-difluoroquinolone-derivatives
#1
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...
March 24, 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
#2
Anita Luethy, James D Boghosian, Rithu Srikantha, Joseph 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
#3
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-inhibition-of-iodothyronine-deiodinase
#4
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 competitively inhibit iodothyronine deiodinases (Dio) by blocking 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 to a methylselenolate model of the Dio active site using density functional theory...
March 10, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28274352/drug-induced-acne
#5
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
#6
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
https://www.readbyqxmd.com/read/28250323/development-of-damaged-nucleoside-mimics-for-inhibition-of-their-repair-enzymes
#7
Yosuke Taniguchi
 8-Oxo-2'-deoxyguanosine (8-oxo-dG) is a representative of nucleoside damage, which is generated by the reaction of the 8 position of dG with reactive oxygen species. Abundant 8-oxo-dG in DNA exhibits genotoxicity and has been linked to aging and disease, such as cancer. As the metabolism of cancer cells is much faster than that of normal cells, the oxidized product of the oligonucleotides and the nucleotide pool produces 8-oxo-dG and 8-oxo-2'-deoxyguanosine triphosphate (8-oxo-dGTP), respectively. Human oxoguanine glycosylase (hOGG1) shows base excision activity for 8-oxo-dG in duplex DNA...
2017: Yakugaku Zasshi: Journal of the Pharmaceutical Society of Japan
https://www.readbyqxmd.com/read/28220538/on-bead-combinatorial-synthesis-and-imaging-of-europium-iii-based-paracest-agents-aids-in-identification-of-chemical-features-that-enhance-cest-sensitivity
#8
Jaspal Singh, Vineeta Rustagi, Shanrong Zhang, A Dean Sherry, D Gomika Udugamasooriya
The rate of water exchange between the inner-sphere of a paramagnetic ion and bulk water is an important parameter in determining the magnitude of the chemical exchange saturation transfer signal from paramagnetic CEST agents (paraCEST). This is governed by various geometric, steric, and ligand field factors created by macrocyclic ligands surrounding the paramagnetic metal ion. Our previous on-bead combinatorial studies of di-peptoid-europium(III)-DOTA-tetraamide complexes revealed that negatively charged groups in the immediate vicinity of the metal center strongly enhances the CEST signal...
February 21, 2017: Magnetic Resonance in Chemistry: MRC
https://www.readbyqxmd.com/read/28203273/synthesis-and-biological-evaluation-of-the-new-1-3-dimethylxanthine-derivatives-with-thiazolidine-4-one-scaffold
#9
Sandra Constantin, Florentina Geanina Lupascu, Maria Apotrosoaei, Ioana Mirela Vasincu, Dan Lupascu, Frederic Buron, Sylvain Routier, Lenuta Profire
BACKGROUND: The xanthine structure has proved to be an important scaffold in the process of developing a wide variety of biologically active molecules such as bronchodilator, hypoglycemiant, anticancer and anti-inflammatory agents. It is known that hyperglycemia generates reactive oxygen species which are involved in the progression of diabetes mellitus and its complications. Therefore, the development of new compounds with antioxidant activity could be an important therapeutic strategy against this metabolic syndrome...
2017: Chemistry Central Journal
https://www.readbyqxmd.com/read/28198903/a-stereoselective-synthesis-of-e-or-z-%C3%AE-arylvinyl-halides-via-a-borylative-coupling-halodeborylation-protocol
#10
Jakub Szyling, Adrian Franczyk, Piotr Pawluć, Bogdan Marciniec, Jędrzej Walkowiak
A new stereoselective method for the synthesis of (E)-β-arylvinyl iodides and (E)- or (Z)-β-arylvinyl bromides from styrenes and vinyl boronates on the basis of a one-pot procedure via borylative coupling/halodeborylation is reported. Depending on the halogenating agent as well as the mode of the halodeborylation reaction, (E) or (Z) isomers are selectively formed.
February 15, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28198170/antibacterial-effect-of-sevoflurane-and-isoflurane
#11
M Martínez-Serrano, M Gerónimo-Pardo, A Martínez-Monsalve, M D Crespo-Sánchez
OBJECTIVE: Multidrug resistant bacteria are increasing worldwide and therapeutic options are limited. Some anaesthetics have shown antibacterial activity before. In this study, we have investigated the antibacterial effect of the halogenated anaesthetic agents sevoflurane and isoflurane against a range of resistant pathogens. METHODS: Two experiments were conducted. In the first, bacterial suspensions of both ATCC and resistant strains of Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa were exposed to liquid sevoflurane and isoflurane during 15, 30 and 60 minutes...
February 15, 2017: Revista Española de Quimioterapia: Publicación Oficial de la Sociedad Española de Quimioterapia
https://www.readbyqxmd.com/read/28177237/direct-c-h-cyanation-of-arenes-via-organic-photoredox-catalysis
#12
Joshua B McManus, David A Nicewicz
Methods for the direct C-H functionalization of aromatic compounds are in demand for a variety of applications, including the synthesis of agrochemicals, pharmaceuticals, and materials. Herein, we disclose the construction of aromatic nitriles via direct C-H functionalization using an acridinium photoredox catalyst and trimethylsilyl cyanide under an aerobic atmosphere. The reaction proceeds at room temperature under mild conditions and has proven to be compatible with a variety of electron-donating and -withdrawing groups, halogens, and nitrogen- and oxygen-containing heterocycles, as well as aromatic-containing pharmaceutical agents...
February 14, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28161088/synthesis-and-qsar-study-of-novel-%C3%AE-methylene-%C3%AE-butyrolactone-derivatives-as-antifungal-agents
#13
Yong-Ling Wu, De-Long Wang, En-Hui Guo, Shuang Song, Jun-Tao Feng, Xing Zhang
Thirty-six new α-benzylidene-γ-lactone compounds based α-methylene-γ-butyrolactone substructure were prepared and characterized by spectroscopic analysis. All compounds were evaluated for antifungal activities in vitro against six plant pathogenic fungi and the half maximal inhibitory concentration (IC50) against Botrytis cinerea and Colletotrichum lagenarium were investigated. Compounds 5c-3 and 5c-5 with the halogen atom exhibited excellent fungicidal activity against B. cinerea (IC50=22.91, 18.89μM)...
January 13, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28133390/influence-of-antimony-halogen-additives-on-flame-propagation
#14
Valeri I Babushok, Peter Deglmann, Roland Krämer, Gregory T Linteris
A kinetic model for flame inhibition by antimony-halogen compounds in hydrocarbon flames is developed. Thermodynamic data for the relevant species are assembled from the literature, and calculations are performed for a large set of additional species of Sb-Br-C-H-O system. The main Sb- and Br-containing species in the combustion products and reaction zone are determined using flame equilibrium calculations with a set of possible Sb-Br-C-H-O species, and these are used to develop the species and reactions in a detailed kinetic model for antimony flame inhibition...
2017: Combust Sci Technol
https://www.readbyqxmd.com/read/28053569/synthesis-of-n-mannich-bases-of-berberine-linking-piperazine-moieties-revealing-anticancer-and-antioxidant-effects
#15
Bhupendra Mistry, Rahul V Patel, Young-Soo Keum, Doo Hwan Kim
A new Mannich base series of piperazine linked berberine analogues was furnished in this study to screen the antioxidant and anticancer potential of the resultant analogues. Alkoxy group at a C-9 position of berberine was converted to hydroxyl functionality to enhance the ability of final scaffolds binding to the target of drug action mainly through hydrophobic effect, conjugation effect, whereas Mannich base functionality was introduced on the C-12 position of berberine. Scaffolds were investigated for their free radical scavenging antioxidant potential in FRAP and DPPH assay, whereas tested to check their Fe(+3) reducing power in ABTS assay...
January 2017: Saudi Journal of Biological Sciences
https://www.readbyqxmd.com/read/28049918/trialkylamine-derivatives-containing-a-triazole-moiety-as-promising-ergosterol-biosynthesis-inhibitor-design-synthesis-and-antifungal-activity
#16
Guoqing Sui, Wen Zhang, Kun Zhou, Yulin Li, Bingyu Zhang, Dan Xu, Yong Zou, Wenming Zhou
As a part of our continuing research on amine derivative antifungal agents, 19 novel target compounds containing 1,2,4-triazole and tertiary amine moieties were designed and synthesized, and their in vitro antifungal activities against six phytopathogenic fungi (Magnaporthe grisea, Alternaria solani, Fusarium solani, Curvularia lunata, A. alternata, F. graminearum) were assayed. All target compounds were elucidated by means of (1)H-NMR, (13)C-NMR, high resolution (HR)-MS, and IR analysis. The results showed that most of the derivatives exhibited obvious activity against each of the fungi at 50 µg/mL...
2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28035962/literature-survey-and-further-studies-on-the-3-alkylation-of-n-unprotected-3-monosubstituted-oxindoles-practical-synthesis-of-n-unprotected-3-3-disubstituted-oxindoles-and-subsequent-transformations-on-the-aromatic-ring
#17
Eszter Kókai, Gyula Simig, Balázs Volk
The paper provides a comprehensive review of the base-catalysed C3-alkylation of N-unprotected-3-monosubstituted oxindoles. Based on a few, non-systematic studies described in the literature using butyllithium as the deprotonating agent, an optimized method has now been elaborated, via the corresponding lithium salt, for the selective C3-alkylation of this family of compounds. The optimal excess of butyllithium and alkylating agent, and the role of the halogen atom in the latter (alkyl bromides vs. iodides) were also studied...
December 26, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/27976495/detection-of-dna-double-strand-breaks-by-pulsed-field-gel-electrophoresis
#18
Yuri Kawashima, Nahomi Yamaguchi, Rie Teshima, Hisashi Narahara, Yoshio Yamaoka, Hirofumi Anai, Yoshihiro Nishida, Katsuhiro Hanada
A DNA double-strand break (DSB) is one of the most cytotoxic DNA lesions because unrepaired DSBs cause chromosomal aberrations and cell death. Although many physiological DSBs occur at DNA replication sites, the molecular mechanisms underlying this remain poorly understood. There was therefore a need to develop a highly specific method to detect DSB fragments containing DNA replication sites. Here we investigated whether pulsed-field gel electrophoresis (PFGE) combined with visualization of DNA replication sites by immunoblotting using halogenized deoxyuridines, such as BrdU and IdU, was sufficient for this detection...
January 2017: Genes to Cells: Devoted to Molecular & Cellular Mechanisms
https://www.readbyqxmd.com/read/27934403/transition-metal-complex-cationic-dyes-photosensitive-to-two-types-of-2d-layered-silver-bromides-with-visible-light-driven-photocatalytic-properties
#19
Cheng-Yang Yue, Xiao-Wu Lei, Yong-Fang Han, Xin-Xiu Lu, Ya-Wei Tian, Jing Xu, Xiao-Fan Liu, Xin Xu
With mixed transition-metal (TM) complex, alkali-metal cations, or halogen anions as structure-directing agents, two types of two-dimensional (2D) layered inorganic-organic hybrid silver bromides were prepared and structurally characterized as K[TM(2,2-bipy)3]2Ag6Br11 (TM = Ni (1), Co (2), Zn (3), Fe (4)) and [TM(2,2-bipy)3]2Ag13Br17 (TM = Ni (5), Co (6), Zn (7), Fe (8)). Compounds 1-4 feature 2D microporous anionic [Ag6Br11](5-) layers composed of [Ag3Br7] secondary building units based on AgBr4 tetrahedral units, and compounds 5-8 contain 2D [Ag13Br16](3-) layers built from the one-dimensional complex [Ag8Br12] and [Ag5Br8] chains...
December 5, 2016: Inorganic Chemistry
https://www.readbyqxmd.com/read/27931386/fate-of-environmental-pollutants
#20
Lokesh P Padhye
This annual review covers the literature published in 2015 on topics related to the occurrence and fate of emerging environmental pollutants in wastewater. Due to the vast amount of literature published on this topic, I have discussed only a fraction of the quality research publications, up to maximum 20 relevant articles per section, due to limitation of space. The abstract search was carried out using Web of Science, and the abstracts were selected based on their relevance. In few cases, full-text articles were referred to better understand new findings...
October 2016: Water Environment Research: a Research Publication of the Water Environment Federation
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