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Richard L Rotundo
Acetylcholinesterase (AChE) is expressed as several homomeric and heterooligomeric forms in a wide variety of tissues such as neurons in the central and peripheral nervous systems and their targets including skeletal muscle, endocrine and exocrine glands. In addition, glycolipid-anchored forms are expressed in erythropoietic and lymphopoietic cells. While transcriptional and post-transcriptional regulation is important for determining which AChE oligomeric forms are expressed in a given tissue, translational and post-translational regulatory mechanisms at the level of protein folding, assembly and sorting play equally important roles in assuring that the AChE molecules reach their intended sites on the cell surface in the appropriate numbers...
March 21, 2017: Journal of Neurochemistry
Pavel Majek, Jan Krupcik, Zachary S Breitbach, Milan K Dissanayake, Peter Kroll, Aaron A Ruch, LeGrande M Slaughter, Daniel W Armstrong
Dynamic high resolution liquid chromatography (DHPLC) was used to determine the kinetic and thermodynamic activation parameters of interconversion of three novel pentahelicene derivatives {3,5-bis(trifluoromethyl)benzo[i]pentahelicene, naphtho[1,2-i]pentahelicene and 4-methoxybenzo[i]pentahelicene}. DHPLC was performed on a chiral isopropyl - carbamate cyclofructan 6 (LARIHC CF6-P) column under normal phase conditions. Variation of the column temperature and flow rate was used to study the interconversion process...
December 21, 2016: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
Arijit A Adhikari, Tamie Suzuki, Reesheda J Gilbert, Matthew R Linaburg, John Daniel Chisholm
The rearrangement of allylic trichloroacetimidates is a well-known transformation, but the corresponding rearrangement of benzylic trichloroacetimidates has not been explored as a method for the synthesis of benzylic amines. Conditions that provide the trichloroacetamide product from a benzylic trichloroacetimidate in high yield have been developed. Methods were also investigated to transform the trichloroacetamide product directly into the corresponding amine, carbamate and urea. A cationic mechanism for the rearrangement is implicated by the available data...
March 21, 2017: Journal of Organic Chemistry
Jeremias E G A Dold, Jessica Pfotzer, Anne-Katrin Späte, Valentin Wittmann
Sialic acids play an important role in numerous cell adhesion processes and sialylation levels are known to be altered under certain pathogenic conditions such as cancer. Metabolic glycoengineering with mannosamine derivatives is a convenient way to introduce non-natural chemical reporter groups into sialylated glycoconjugates offering the opportunity to label sialic acids using bioorthogonal ligation chemistry. The labeling intensity not only depends on the rate of the ligation reaction but also on the extent to which the natural sialic acids are replaced by the modified ones, i...
March 20, 2017: Chembiochem: a European Journal of Chemical Biology
Siti Aisyah Nabilah Suwardi, See Mun Lee, Kong Mun Lo, Mukesh M Jotani, Edward R T Tiekink
The title compound, [Cd2(C8H8NS2)4], is a centrosymmetric dimer with both chelating and μ2-tridentate di-thio-carbamate ligands. The resulting S5 donor set defines a Cd(II) coordination geometry inter-mediate between square-pyramidal and trigonal-bipyramidal, but tending towards the former. The packing features C-H⋯S and C-H⋯π inter-actions, which generate a three-dimensional network. The influence of these inter-actions, along with intra-dimer π-π inter-actions between chelate rings, has been investigated by an analysis of the Hirshfeld surface...
March 1, 2017: Acta Crystallographica. Section E, Crystallographic Communications
Fuyuhiko Inagaki, Chiaki Matsumoto, Takashi Iwata, Chisato Mukai
Emission gas and air contain not only CO2 but also plentiful moisture, making it difficult to achieve selective CO2 absorption without hydration. To generate absorbed CO2 (wet CO2) under heating, the need for external energy to release the absorbed water has been among the most serious problems in the fields of carbon dioxide capture and storage (CCS) and direct air capture (DAC). We found that the introduction of the hydrophobic phenyl group into alkylamines of CO2 absorbents improved the absorption selectivity between CO2 and water...
March 17, 2017: Journal of the American Chemical Society
Azusa Kondoh, Yuji Kamata, Masahiro Terada
An efficient synthesis of enantioenriched γ-amino-α,β-unsaturated esters was developed by utilizing the palladium-catalyzed decarboxylative rearrangement of enantioenriched allylic carbamates possessing an ester moiety at the allylic position. The reaction proceeded in good yield with a high degree of chirality transfer by making use of Xantphos as a superior ligand for the catalyst. The products directly participated in the formal [3 + 2] cycloaddition reaction with tosyl isocyanate under Brønsted base catalysis to afford enantioenriched β,γ-diamino acid derived imidazolidin-2-ones as versatile chiral building blocks...
March 17, 2017: Organic Letters
Hany Fakhry Anwar, Mioara Andrei, Kjell Undheim
Chemoselective substitutions in the C10-methyl group of erythromycin A ketolides is reported. The C10-methyl group in the clarithromycin derived substrate 10,11-anhydro-O(6)-methyl-descladinosylerythromycin was activated by conversion into an allyl acetate and thereafter to the corresponding allylic cyanide. Both the allylic acetate and the cyanide reacted with carbonyldiimidazole and ammonia to afford a C11,C12-cyclic carbamate with concurrent elimination of the allylic function to yield a methylene α,β-unsaturated ketone...
February 23, 2017: Bioorganic & Medicinal Chemistry
Sinyee Gan, Sarani Zakaria, Chin Hua Chia, Ruey Shan Chen, Amanda V Ellis, Hatika Kaco
Here, a stable derivative of cellulose, called cellulose carbamate (CC), was produced from Kenaf (Hibiscus cannabinus) core pulp (KCP) and urea with the aid of a hydrothermal method. Further investigation was carried out for the amount of nitrogen yielded in CC as different urea concentrations were applied to react with cellulose. The effect of nitrogen concentration of CC on its solubility in a urea-alkaline system was also studied. Regenerated cellulose products (hydrogels and aerogels) were fabricated through the rapid dissolution of CC in a urea-alkaline system...
2017: PloS One
Hu-Lin Jiang, Mohammad Ariful Islam, Lei Xing, Jannatul Firdous, Wuji Cao, Yu-Jing He, Yong Zhu, Ki-Hyun Cho, Hui-Shan Li, Chong-Su Cho
Gene therapy using recombinant DNA or gene silencing using siRNA have become a prominent area of research in cancer therapy. However, their use in clinical applications is limited due to overall safety concerns and suboptimal efficacy. Although non-viral vectors such as polycationic polymers do not offer the same level of transfection efficiency as their viral counterparts, they still demonstrate immense potential as alternatives to viral vectors, given their versatility, low immunogenicity, ease of large-scale production, and ability to accelerate gene transfer with well-designed delivery platforms...
April 2017: Topics in Current Chemistry (Journal)
Judith Jeske, Björn Windshügel, Wolfgang E Thasler, Matthias Schwab, Oliver Burk
Unintentional activation of xenosensing nuclear receptors pregnane X receptor (PXR) and/or constitutive androstane receptor (CAR) by clinical drug use is known to produce severe side effects in patients, which may be overcome by co-administering antagonists. However, especially antagonizing CAR is hampered by the lack of specific inhibitors, which do not activate PXR. Recently, compounds based on a dibenzazepine carbamate scaffold were identified as potent CAR inhibitors. However, their potential to activate PXR was not thoroughly investigated, even if the lead compound was named "CAR inhibitor not PXR activator 1" (CINPA1)...
March 13, 2017: Archives of Toxicology
Frapiccini Emanuela, Scarcella Giuseppe, Guicciardi Stefano, Betti Mattia, Marini Mauro
Organochlorines and carbamates are common pesticides predominantly employed in agriculture. Large amounts of pesticides make their way into rivers and marine habitats. They accumulate in aquatic organisms through different exposure routes and gradually move up the food chain. Since contaminant bioaccumulation in animals is affected by several factors, this work harnessed several different approaches to explore the persistence of lindane, a long banned organochlorine pesticide, and carbaryl, a newer generation pesticide, in common sole (Solea solea), a major commercial species in Adriatic fisheries...
March 13, 2017: Bulletin of Environmental Contamination and Toxicology
Quan Gan, Xiang Wang, Brice Kauffmann, Frédéric Rosu, Yann Ferrand, Ivan Huc
At the molecular level, translation refers to the production of a new entity according to a template that has a different chemical composition. In this way, chemical information may be translated from one molecule to another. The process is useful to synthesize structures and thus functions that might be difficult to create otherwise, and it reaches exquisite levels of efficiency in biological systems, as illustrated by protein expression from mRNA templates or by the assembly of the tobacco mosaic virus capsid protein according to the length of its RNA...
March 13, 2017: Nature Nanotechnology
Alfonso D Lovato Echeverria, Susana A Gutiérrez, Marcelo A Carmona
The aim of this study was to evaluate in vitro the mycelial susceptibility of Trichoconiella padwickii to different active ingredients through average median concentration IC50 calculation. Inoculum disks were seeded on bean agar at different concentrations (0.1; 1; 10; 30, 50; 100 and 1000mg/l) of various fungicides. After seven days the colony diameter was measured. The data obtained were fitted to nonlinear regression models. Susceptibility was classified using the scale proposed by Edgington. The results show that the pathogen is very sensitive to products that act on the respiratory chain (quinone outside inhibitors [QoI] and succinate dehydrogenase inhibitors [SDHI]) and cell membrane (multi-site contact activity), and moderately sensitive to those products interfering with cell division (methyl benzimidazole carbamates [MBC]), synthesis of nucleic acids (phenylamides [PA]) and osmotic signal transduction (multi-site contact activity)...
March 8, 2017: Revista Argentina de Microbiología
Filipa C Santos, Ana M S Soares, M Sameiro T Gonçalves, Susana P G Costa
Ala-Ala-Pro-Val (AAPV) is a bioactive tetrapeptide that inhibits human neutrophil elastase, an enzyme involved in skin chronic inflammatory diseases like psoriasis. Caged derivatives of this peptide were prepared by proper N- and C-terminal derivatisation through a carbamate or ester linkage, respectively, with two photoactive moieties, namely 7-methoxycoumarin-2-ylmethyl and pyren-2-ylmethyl groups. These groups were chosen to assess the influence of the photosensitive group and the type of linkage in the controlled photo release of the active molecule...
March 10, 2017: Amino Acids
Bin Yang, Kantapat Chansaenpak, Hongmiao Wu, Lin Zhu, Mengzhe Wang, Zibo Li, Hongjian Lu
The intramolecular fluorocyclization of unsaturated carbamates is described here using a hypervalent iodine reagent in the presence of a silver catalyst. Both (hetero)aryl-substituted olefins and acrylamides can be utilized as effective substrates. Preliminary mechanistic investigations suggest that the reaction proceeds via a cyclization/1,2-(hetero)aryl migration/fluorination cascade involving an unusual radical process. Furthermore, starting from no-carrier-added [(18)F]TBAF, a simple one-pot, two-step cascade method was developed for the generation of (18)F-labeled heterocycles with high radiochemical purity...
March 10, 2017: Chemical Communications: Chem Comm
Simon Peguedwinde Sawadogo, Abdoulaye Niang, Etienne Bilgo, Azize Millogo, Hamidou Maïga, Roch K Dabire, Frederic Tripet, Abdoulaye Diabaté
Malaria control programs are being jeopardized by the spread of insecticide resistance in mosquito vector populations. It has been estimated that the spread of resistance could lead to an additional 120000 deaths per year, and interfere with the prospects for sustained control or the feasibility of achieving malaria elimination. Another complication for the development of resistance management strategies is that, in addition to insecticide resistance, mosquito behavior evolves in a manner that diminishes the impact of LLINs and IRS...
2017: PloS One
Li Chia Chong, Tabitha Healey, Tony Michele, Timothy J Price
Standard treatment for locally advanced anal cancer is chemoradiotherapy with mitomycin C and fluorouracil. However, infusional fluorouracil requires central venous catheter placement potentiating risk of infection and thrombosis. Capecitabine which is an oral tumor activated fluoropyrimidine carbamate is an established treatment alternative to infusional fluorouracil for patients with gastrointestinal cancers. Areas covered: This review examines and discusses the current evidence for substitution of Capecitabine for infusional fluorouracil in locally advanced anal cancer...
March 13, 2017: Expert Review of Anticancer Therapy
David Bibi, Hafiz Mawasi, Alessio Nocentini, Claudiu T Supuran, Bogdan Wlodarczyk, Richard H Finnell, Meir Bialer
Epilepsy is one of the most common neurological diseases, with between 34 and 76 per 100,000 people developing epilepsy annually. Epilepsy therapy for the past 100(+) years is based on the use of antiepileptic drugs (AEDs). Despite the availability of more than twenty old and new AEDs, approximately 30% of patients with epilepsy are not seizure-free with the existing medications. In addition, the clinical use of the existing AEDs is restricted by their side-effects, including the teratogenicity associated with valproic acid that restricts its use in women of child-bearing age...
March 9, 2017: Neurochemical Research
Qiong Xie, Zhaoxi Zheng, Biyun Shao, Wei Fu, Zheng Xia, Wei Li, Jian Sun, Wei Zheng, Weiwei Zhang, Wei Sheng, Qihong Zhang, Hongzhuan Chen, Hao Wang, Zhuibai Qiu
Multifunctional carbamate-type acetylcholinesterase (AChE) inhibitors with anti-amyloidogenic properties like phenserine are potential therapeutic agents for Alzheimer's disease (AD). We reported here the design of new carbamates using pharmacophore model strategy to modulate both cholinesterase and amyloidogenesis. A five-feature pharmacophore model was generated based on 25 carbamate-type training set compounds. (-)-Meptazinol carbamates that superimposed well upon the model were designed and synthesized, which exhibited nanomolar AChE inhibitory potency and good anti-amyloidogenic properties in in vitro test...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
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