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Carbamate

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https://www.readbyqxmd.com/read/28441501/hooked-on-cryogels-a-carbamate-linker-based-depot-for-slow-drug-release
#1
Duygu Aydin, Mehmet Arslan, Amitav Sanyal, Rana Sanyal
Poly(ethylene glycol) (PEG) based bulk hydrogels and cryogels containing activated carbonate groups as amine reactive handles to facilitate drug conjugations through carbamate linkages were fabricated and evaluated as slow releasing drug reservoirs. As an initial approach, photopolymerization of N-hydroxysuccinimide (NHS)-activated carbonate functional group containing monomer and PEG-methacrylate in the presence of a crosslinker was utilized to obtain bulk hydrogels with high gel conversions. The resultant hydrogels possessed moderate water uptake (170-340 %) which was dependent on the monomer ratios...
April 25, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/28440824/phi-oac-2-mediated-1-2-aminohalogenation-of-alkynes-a-general-access-to-e-4-halomethylene-oxazolidin-2-ones
#2
RuiJia Wang, Huaxu Zou, Yi Xiong, Niannian Yi, Wei Deng, Jiannan Xiang
A new PhI(OAc)2-mediated 1,2-aminohalogenation of prop-2-yn-1-yl carbamates and various halogen sources is presented with excellent selectivity and high step-economy. The reaction is general and rapid for the construction of diverse (E)-4-(halomethylene)oxazolidin-2-ones through the generation of the three-membered ring or N-radical followed by intramolecular cyclization.
April 25, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28435704/a-two-dimensional-coordination-polymer-poly-bis-%C3%AE-2-n-ethyl-n-pyridin-4-ylmeth-yl-di-thio-carbamato-%C3%AE%C2%BA-3-n-s-s-cadmium-ii-3-methyl-pyridine-monosolvate
#3
Hadi D Arman, Pavel Poplaukhin, Edward R T Tiekink
The title compound, {[Cd(C9H11N2S2)2]·C6H7N} n , features two μ2-κ(3)-di-thio-carbamate ligands each of which chelates one Cd(II) atom, via the S atoms, while simultaneously bridging to another via the pyridyl-N atom. The result is a two-dimensional coordination polymer extending parallel to the ab plane with square channels along the b axis. The Cd(II) atom geometry is based on a distorted cis-N2S4 octa-hedron. The 3-methyl-pyridine mol-ecules reside in the channels aligned along the b axis, being held in place by methyl-ene-C-H⋯N(3-methyl-pyridine) and (3-methyl-pyridine)-C-H⋯π(pyrid-yl) inter-actions...
April 1, 2017: Acta Crystallographica. Section E, Crystallographic Communications
https://www.readbyqxmd.com/read/28433778/novel-lipid-mimetic-prodrugs-delivering-active-compounds-to-adipose-tissue
#4
Andrea Mattarei, Andrea Rossa, Veronica Bombardelli, Michele Azzolini, Martina La Spina, Cristina Paradisi, Mario Zoratti, Lucia Biasutto
Obesity and associated pathologies are a dramatically growing problem. New therapies to prevent and/or cure them are strongly needed. Adipose tissue is a logical target for pharmacological intervention, since it is now recognized to exert an important endocrine function, secreting a variety of adipokines affecting, for example, adiposity and insulin resistance. This proof of principle work focuses on the development of novel lipid-mimetic prodrugs reaching fat deposits by the same lymphatic absorption route followed by dietary triglycerides...
April 13, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28428243/genome-wide-transcription-and-functional-analyses-reveal-heterogeneous-molecular-mechanisms-driving-pyrethroids-resistance-in-the-major-malaria-vector-anopheles-funestus-across-africa
#5
Jacob M Riveron, Sulaiman S Ibrahim, Charles Mulamba, Rousseau Djouaka, Helen Irving, Murielle J Wondji, Intan H Ishak, Charles S Wondji
Pyrethroid resistance in malaria vector, An. Funestus is increasingly reported across Africa, threatening the sustainability of pyrethroid-based control interventions including long lasting insecticidal Nets (LLINs). Managing this problem requires understanding of the molecular basis of the resistance from different regions of the continent, to establish whether it is being driven by a single or independent selective events. Here, using a genome-wide transcription profiling of pyrethroid resistant populations from Southern (Malawi), East (Uganda) and West Africa (Benin), we investigated the molecular basis of resistance, revealing strong differences between the different African regions...
April 19, 2017: G3: Genes—Genomes—Genetics
https://www.readbyqxmd.com/read/28427415/insecticide-resistance-patterns-in-uganda-and-the-effect-of-indoor-residual-spraying-with-bendiocarb-on-kdr-l1014s-frequencies-in-anopheles-gambiae-s-s
#6
Tarekegn A Abeku, Michelle E H Helinski, Matthew J Kirby, James Ssekitooleko, Chris Bass, Irene Kyomuhangi, Michael Okia, Godfrey Magumba, Sylvia R Meek
BACKGROUND: Resistance of malaria vectors to pyrethroid insecticides has been attributed to selection pressure from long-lasting insecticidal nets (LLINs), indoor residual spraying (IRS), and the use of chemicals in agriculture. The use of different classes of insecticides in combination or by rotation has been recommended for resistance management. The aim of this study was to understand the role of IRS with a carbamate insecticide in management of pyrethroid resistance. METHODS: Anopheles mosquitoes were collected from multiple sites in nine districts of Uganda (up to five sites per district)...
April 20, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28425184/enantioselective-synthesis-of-mitomycin%C3%A2-k-by-a-palladium-catalyzed-oxidative-tandem-cyclization
#7
Qiang-Shuai Gu, Dan Yang
The mitomycins, a family of bioactive natural products, feature a compact 6/5/5-fused polycyclic ring structure densely decorated with highly reactive and/or fragile quinone, amino ketal, and aziridine as well as carbamate moieties. It is this striking feature that has defeated numerous synthetic attempts towards these apparently small molecules, rendering them one of the most formidable targets for total synthesis. We herein report the first enantioselective synthesis of (+)-mitomycin K, a representative of G series mitomycins...
April 20, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28423990/self-assembled-nanogel-of-cholesterol-bearing-xyloglucan-as-a-drug-delivery-nanocarrier
#8
Shin-Ichi Sawada, Hiroko Yukawa, Shigeo Takeda, Yoshihiro Sasaki, Kazunari Akiyoshi
Xyloglucan (XG) is a multibranched polysaccharide consisting of a main chain β-1,4-glucan with xylose and galactose side chains. In this study, cholesterol-bearing XG (CHXG) was synthesized by the reaction of XG with cholesteryl N- (6-isocyanatohexyl) carbamate. The CHXG molecules self-assembled in water to form nanogels consisting of about 100 molecules of XG, and were characterized using differential light scattering and transmission electron microscopy. The number of cholesteryl groups per physical cross-linking site was estimated using a fluorescence quenching method...
April 20, 2017: Journal of Biomaterials Science. Polymer Edition
https://www.readbyqxmd.com/read/28421757/a-bulky-disulfoxide-ligand-for-pd-catalyzed-oxidative-allylic-c-h-amination-with-2-2-2-trichloroethyl-tosyl-carbamate
#9
You-Gui Li, Li Li, Ming-Yue Yang, Gang He, Eric Assen B Kantchev
Challenging substrates and conditions in homogeneous catalysis pose stringent demands on the ligands used. A novel, bulky, 1-adamantyl-substituted disulfoxide ligand designed after a systematic evaluation of the electronic and steric properties of disulfoxide substituents permits the allylic oxidative C-N coupling reaction to proceed at lower catalyst loading while requiring a smaller excess of reagents. Additionally, this ligand improves the yields when TsNHCOOCH2CCl3, a novel reagent that permits deprotection of the products under both acidic and basic conditions, is used...
April 26, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28418831/the-evaluation-of-benefit-of-newly-prepared-reversible-inhibitors-of-acetylcholinesterase-and-commonly-used-pyridostigmine-as-pharmacological-pretreatment-of-soman-poisoned-mice
#10
Jiří Kassa, Jan Korábečný, Eugenie Nepovimová
AIM: The ability of four newly prepared reversible inhibitors of acetylcholinesterase (6-chlorotacrine, 7-phenoxytacrine, compounds 1 and 2) and currently used carbamate pyridostigmine to increase the resistance of mice against soman and the efficacy of antidotal treatment of soman-poisoned mice was evaluated. METHODS: The evaluation of the effect of pharmacological pretreatment is based on the identification of changes of soman-induced toxicity that was evaluated by the assessment of its LD50 value and its 95% confidence limit using probitlogarithmical analysis of death occurring within 24 h after administration of soman...
April 18, 2017: Acta Medica (Hradec Králové)
https://www.readbyqxmd.com/read/28418299/control-of-malaria-vector-mosquitoes-by-insecticide-treated-combinations-of-window-screens-and-eave-baffles
#11
Gerry F Killeen, John P Masalu, Dingani Chinula, Emmanouil A Fotakis, Deogratius R Kavishe, David Malone, Fredros Okumu
We assessed window screens and eave baffles (WSEBs), which enable mosquitoes to enter but not exit houses, as an alternative to indoor residual spraying (IRS) for malaria vector control. WSEBs treated with water, the pyrethroid lambda-cyhalothrin, or the organophosphate pirimiphos-methyl, with and without a binding agent for increasing insecticide persistence on netting, were compared with IRS in experimental huts. Compared with IRS containing the same insecticide, WSEBs killed similar proportions of Anopheles funestus mosquitoes that were resistant to pyrethroids, carbamates and organochlorines and greater proportions of pyrethroid-resistant, early exiting An...
May 2017: Emerging Infectious Diseases
https://www.readbyqxmd.com/read/28411311/total-fluorescence-fingerprinting-of-pesticides-a-reliable-approach-for-continuous-monitoring-of-soils-and-waters
#12
Hicham Hassoun, Taibi Lamhasni, Salim Foudeil, Abdelmajid El Bakkali, Saadia Ait Lyazidi, Mustapha Haddad, M'barek Choukrad, Mohamed Hnach
The present work relates to the creation/extension of a database of Total Excitation-Emission and Total Synchronous Fluorescence Matrices (TEEMs and TSFMs) along with optimal Synchronous Fluorescence Spectra (SFS) to fingerprint pesticides widely used in Morocco. This spectrometric multi-component fingerprinting may permit the direct detection of pesticides persisting in soil or water. The objective of the current investigation is to detect four pesticide remains in agricultural soils by applying the spectrometric fingerprinting results...
April 14, 2017: Journal of Fluorescence
https://www.readbyqxmd.com/read/28410869/effect-of-natural-and-semi-synthetic-cadinanes-from-heterotheca-inuloides-on-nf-%C3%AE%C2%BAb-nrf2-and-stat3-signaling-pathways-and-evaluation-of-their-in-vitro-cytotoxicity-in-human-cancer-cell-lines
#13
Verónica Egas, Estrella Millán, Juan A Collado, Teresa Ramírez-Apan, Carlos A Méndez-Cuesta, Eduardo Muñoz, Guillermo Delgado
The effects of ten natural cadinane sesquiterpenoids isolated from Heterotheca inuloides on the pathways of the NF-κB, Nrf2 and STAT3 transcription factors were studied for the first time. The main constituent in this species, 7-hydroxy-3,4-dihydrocadalene (1), showed anti-NF-κB activity and activated the antioxidant Nrf2 pathway, which may explain the properties reported for the traditional use of the plant. In addition to the main metabolite, a structurally similar compound, 7-hydroxy-cadalene (2), also displayed anti-NF-κB activity...
April 2, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28407955/influence-of-ripeness-and-maceration-of-the-grapes-on-levels-of-furan-and-carbonyl-compounds-in-wine-simultaneous-quantitative-determination-and-assessment-of-the-exposure-risk-to-these-compounds
#14
Laura Oliveira Lago, Karine Primieri Nicolli, Aline Biasoto Marques, Claudia Alcaraz Zini, Juliane Elisa Welke
The validated method based on the use of headspace solid phase microextraction (HS-SPME) coupled with the comprehensive two-dimensional gas chromatography with time-of-flight mass spectrometric detection (GC×GC/TOFMS) proved to be appropriate for this first simultaneous quantitative determination of six toxic compounds (formaldehyde, acetaldehyde, ethyl carbamate, furan, furfural and acrolein) found in wines. Acetaldehyde and acrolein coeluted with other wine compounds, which indicated that difficulties could arise if only one-dimensional gas chromatography was used for the determination of these compounds...
September 1, 2017: Food Chemistry
https://www.readbyqxmd.com/read/28407384/point-mutations-in-acetylcholinesterase-1-associated-with-chlorpyrifos-resistance-in-the-brown-planthopper-nilaparvata-lugens-st%C3%A3-l
#15
Y Zhang, B Yang, J Li, M Liu, Z Liu
Insecticide resistance frequently results from target-site insensitivity, such as point mutations in acetylcholinesterases (AChEs) for resistance to organophosphates and carbamates. From a field-originated population of Nilaparvata lugens, a major rice pest, a resistant population (R9) was obtained by nine-generation continuous selection with chlorpyrifos. From the same field population, a relatively susceptible population (S9) was also constructed through rearing without any insecticides. Compared to the susceptible strain, Sus [medium lethal dose (LC50 ) = 0...
April 13, 2017: Insect Molecular Biology
https://www.readbyqxmd.com/read/28406544/halogen-free-synthesis-of-carbamates-from-co2-and-amines-using-titanium-alkoxides
#16
Jun-Chul Choi, Hao-Yu Yuan, Norihisa Fukaya, Syun-Ya Onozawa, Qiao Zhang, Seong Jib Choi, Hiroyuki Yasuda
The direct synthesis of carbamates from amines and carbon dioxide in the presence of Ti(OR)4 (R = nBu (1), Me (2), Et (3), nPr (4)) was investigated. Aniline was reacted with the titanium n-butoxide (1) in the presence of carbon dioxide (5 MPa) to give the corresponding n-butyl N-phenylcarbamate (BPC) in nearly quantitative yield (99%) within 20 min. Furthermore, 1 could be regenerated upon reaction with n-butanol during water removal. The recovered 1 could then be reused in a subsequent reaction.
April 12, 2017: Chemistry, An Asian Journal
https://www.readbyqxmd.com/read/28398497/detection-of-reduced-susceptibility-to-chlorfenapyr-and-bifenthrin-containing-products-in-field-populations-of-the-bed-bug-hemiptera-cimicidae
#17
Aaron R Ashbrook, Michael E Scharf, Gary W Bennett, Ameya D Gondhalekar
Insecticide resistance is a major impediment for effective control of Cimex lectularius L. Previous resistance detection studies with bed bugs have focused on certain pyrethroid, neonicotinoid, organochlorine, organophosphate, and carbamate insecticides. Within the pyrethroid class, resistance studies have mostly been limited to deltamethrin, lambda-cyhalothrin, and alpha- and beta-cyfluthrin. The goal of this study was to develop diagnostic concentration bioassays for assessing bed bug susceptibility levels to chlorfenapyr- and bifenthrin-containing products...
April 10, 2017: Journal of Economic Entomology
https://www.readbyqxmd.com/read/28398240/anti-inflammatory-antioxidant-and-crystallographic-studies-of-n-palmitoyl-ethanol-amine-pea-derivatives
#18
Carmela Saturnino, Ada Popolo, Anna Ramunno, Simona Adesso, Michela Pecoraro, Maria Rosaria Plutino, Silvia Rizzato, Alberto Albinati, Stefania Marzocco, Marina Sala, Domenico Iacopetta, Maria Stefania Sinicropi
N-Palmitoyl-ethanolamine (PEA) is an anti-inflammatory component of egg yolk that is usually employed for the prevention of respiratory apparatus virus infection and then frequently used for its efficient anti-inflammatory and analgesic effects in experimental models of visceral, neuropathic, and inflammatory diseases. Nevertheless, data of its use in animal or human therapy are still scarce and further studies are needed. Herein, we report the biological evaluation of a small library of N-palmitoyl-ethanolamine analogues or derivatives, characterized by a protected acid function (either as palmitoyl amides or hexadecyl esters), useful to decrease their hydrolysis rate in vitro and prolong their biological activity...
April 11, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28387416/transition-metal-free-synthesis-of-1-1-diboronate-esters-with-a-fully-substituted-benzylic-center-via-diborylation-of-lithiated-carbamates
#19
Haonan Zhao, Min Tong, Haijun Wang, Senmiao Xu
A transition-metal-free lithiation-borylation method has been developed to access a variety of 1,1-diboronate esters with a fully substituted benzylic center from readily available secondary benzylic N,N-diisopropyl carbamates. The method is applicable to scale-up synthesis of 1,1-diboron compounds. Furthermore, the current method is also applicable to synthesizing optically active 1,1-silylboronate esters.
April 18, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28385577/carbamates-and-ich-m7-classification-making-use-of-expert-knowledge
#20
Rachel Hemingway, Adrian Fowkes, Richard V Williams
Carbamates are widely used in the chemical industry so understanding their toxicity is important to safety assessment. Carbamates have been associated with certain toxicities resulting in publication of structural alerts, including alerts for mutagenicity. Structural alerts for bacterial mutagenicity can be used in combination with statistical systems to enable ICH M7 classification, which allows assessment of the genotoxic risk posed by pharmaceutical impurities. This study tested a hypothetical bacterial mutagenicity alert for carbamates and examined the impact it would have on ICH M7 classifications using QSAR predictions from the expert rule-based system Derek Nexus and the statistical-based system Sarah Nexus...
April 3, 2017: Regulatory Toxicology and Pharmacology: RTP
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