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https://www.readbyqxmd.com/read/29347906/expression-and-functional-analysis-of-the-propamocarb-related-gene-csdir16-in-cucumbers
#1
Chunhong Liu, Zhiwei Qin, Xiuyan Zhou, Ming Xin, Chunhua Wang, Dong Liu, Shengnan Li
BACKGROUND: Cucumber downy mildew is among the most important diseases that can disrupt cucumber production. Propamocarb, also known as propyl-[3-(dimethylamino)propyl]carbamate (PM), is a systemic carbamate fungicide pesticide that is widely applied in agricultural production because of its high efficiency of pathogens control, especially cucumber downy mildew. However, residual PM can remain in cucumbers after the disease has been controlled. To explore the molecular mechanisms of PM retention, cucumber cultivars 'D9320' (with the highest residual PM content) and 'D0351' (lowest residual PM content) were studied...
January 18, 2018: BMC Plant Biology
https://www.readbyqxmd.com/read/29342859/multinuclear-nmr-measurements-and-dft-calculations-for-capecitabine-tautomeric-form-assignment-in-a-solution
#2
Piotr Cmoch, Piotr Krzeczyński, Andrzej Leś
The molecular structure of capecitabine (a widely applied prodrug of 5-fluorouracil) was studied by multinuclear NMR measurements and DFT quantum mechanical calculations. One or two tautomeric forms in a solution were detected depending on the solvent used. In the organic solvents, a mixture of two forms of capecitabine was observed: carbamate and imine tautomers. In the aqueous solution, only the carbamate form was found. The methylation of capecitabine yields mainly two products in different proportions: N³-methylcapecitabine and N⁷-methylcapecitabine...
January 13, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29335658/highly-stereoselective-asymmetric-aldol-routes-to-tert-butyl-2-3-5-difluorophenyl-1-oxiran-2-yl-ethyl-carbamates-building-blocks-for-novel-protease-inhibitors
#3
Arun K Ghosh, Emilio L Cárdenas, Margherita Brindisi
Enantioselective syntheses of tert-butyl ((S)-2-(3,5-difluorophenyl)-1-((S)-oxiran-2-yl)ethyl)carbamate and ((S)-2-(3,5-difluorophenyl)-1-((R)-oxiran-2-yl)ethyl)carbamate are described. We utilized asymmetric syn- and anti-aldol reactions to set both stereogenic centers. We investigated ester-derived Ti-enolate aldol reactions as well as Evans' diastereoselective syn-aldol reaction for these syntheses. We have converted optically active ((S)-2-(3,5-difluorophenyl)-1-((S)-oxiran-2-yl)ethyl)carbamate to a potent β-secretase inhibitor...
October 25, 2017: Tetrahedron Letters
https://www.readbyqxmd.com/read/29335200/discovery-and-optimization-of-phthalazinone-derivatives-as-a-new-class-of-potent-dengue-virus-inhibitors
#4
Dong Lu, Jianan Liu, Yunzhe Zhang, Feifei Liu, Limin Zeng, Runze Peng, Li Yang, Huazhou Ying, Wei Tang, Wuhong Chen, Jianping Zuo, Xiankun Tong, Tao Liu, Youhong Hu
Using a dengue replicon cell line-based screening, we identified 3-(dimethylamino)propyl(3-((4-(4-fluorophenyl)-1-oxophthalazin-2(1H)-yl)methyl)phenyl)carbamate (10a) as a potent DENV-2 inhibitor, with an IC50 value of 0.64 μM. A series of novel phthalazinone derivatives based on hit 10a were synthesized and evaluated for their in vitro anti-DENV activity and cytotoxicity. The subsequent SAR study and optimization led to the discovery of the most promising compound 14l, which displayed potent anti-DENV-2 activity, with low IC50 value against DENV-2 RNA replication of 0...
January 5, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29333693/polypeptide-polymer-brushes-by-light-induced-surface-polymerization-of-amino-acid-n-carboxyanhydrides
#5
Timo Stukenkemper, Xavier Paquez, M W G M Verhoeven, Emiel J M Hensen, Aylvin A Dias, Dermot F Brougham, Andreas Heise
Silicon wafers are decorated with photoamine generator 4,5-dimethoxy-2-nitrobenzyl 3-(triethoxysilyl)propyl carbamate. UV-irradiation in the presence of benzyl-l-glutamate N-carboxyanhydride is carried out, resulting in the release of the surface-bound primary amines, making them viable N-carboxyanhydride (NCA) polymerization initiators. Successful polypeptide grafting is confirmed by water contact angle measurements as well as by ellipsometry, revealing a poly(benzyl-l-glutamate) (PBLG) layer of ≈3 nm. X-ray photoelectron spectroscopy confirms the presence of amide groups in the grafted PBLG while time-of-flight secondary ion mass spectroscopy provides additional evidence for the presence of PBLG on the surface...
January 15, 2018: Macromolecular Rapid Communications
https://www.readbyqxmd.com/read/29332674/sleep-apnea-and-pesticide-exposure-in-a-study-of-us-farmers
#6
Brittney O Baumert, Megan Ulmer Carnes, Jane A Hoppin, Chandra L Jackson, Dale P Sandler, Laura Beane Freeman, Paul K Henneberger, David M Umbach, Srishti Shrestha, Stuart Long, Stephanie J London
INTRODUCTION: Carbamate and organophosphate pesticides inhibit acetylcholinesterase, and poisoning leads to respiratory depression. Thus, involvement in sleep apnea is plausible, but no data exist at lower levels of exposure. Other pesticides could impact sleep apnea by different mechanisms but have not been studied. Our study examines the associations between pesticide exposure and sleep apnea among pesticide applicators from a US farming population. PARTICIPANTS AND METHODS: We analyzed data from 1569 male pesticide applicators, mostly farmers, from an asthma case-control study nested within the prospective Agricultural Health Study...
February 2018: Sleep Health
https://www.readbyqxmd.com/read/29331685/nucleic-adaptability-of-heterokaryons-to-fungicides-in-a-multinucleate-fungus-sclerotinia-homoeocarpa
#7
Dylan Kessler, Hyunkyu Sang, Amanda Bousquet, Jonathan P Hulvey, Dawlyn Garcia, Siyeon Rhee, Yoichiro Hoshino, Toshihiko Yamada, Geunhwa Jung
Sclerotinia homoeocarpa is the causal organism of dollar spot in turfgrasses and is a multinucleate fungus with a history of resistance to multiple fungicide classes. Heterokaryosis gives rise to the coexistence of genetically distinct nuclei within a cell, which contributes to genotypic and phenotypic plasticity in multinucleate fungi. We demonstrate that field isolates, resistant to either a demethylation inhibitor or methyl benzimidazole carbamate fungicide, can form heterokaryons with resistance to each fungicide and adaptability to serial combinations of different fungicide concentrations...
January 10, 2018: Fungal Genetics and Biology: FG & B
https://www.readbyqxmd.com/read/29329887/determination-of-n-glycans-by-high-performance-liquid-chromatography-using-6-aminoquinolyl-n-hydroxysuccinimidyl-carbamate-as-the-glycosylamine-labeling-reagent
#8
Yike Wu, Qiuyue Sha, Juan Du, Chang Wang, Liang Zhang, Bi-Feng Liu, Yawei Lin, Xin Liu
Robust, efficient identification and accurate quantification of N-glycans are of great significance in N-glycomics analysis. Here, a simple and rapid derivatization method, based on the combination of microwave-assisted deglycosylation and 6-aminoquinolyl-N-hydroxysuccinimidyl carbamate (AQC) labeling, was developed for the analysis of N-glycan by high performance liquid chromatography with fluorescence detection (HPLC-FLD). After optimizing various parameters affecting deglycosylation and derivatization by RNase B, the time for N-glycan labeling was shortened to 50 min with ∼10-fold enhancement in detection sensitivity comparing to conventional 2-aminobenzoic acid (2-AA) labeling method...
January 8, 2018: Journal of Chromatography. A
https://www.readbyqxmd.com/read/29329860/ethyl-carbamate-an-emerging-food-and-environmental-toxicant
#9
REVIEW
Vemana Gowd, Hongming Su, Petr Karlovsky, Wei Chen
Ethyl carbamate (EC), a chemical substance widely present in fermented food products and alcoholic beverages, has been classified as a Group 2A carcinogen by the International Agency for Research on Cancer (IARC). New evidence indicates that long-term exposure to EC may cause neurological disorders. Formation of EC in food and its metabolism have therefore been studied extensively and analytical methods for EC in various food matrices have been established. Due to the potential threat of EC to human health, mitigation strategies for EC in food products by physical, chemical, enzymatic, and genetic engineering methods have been developed...
May 15, 2018: Food Chemistry
https://www.readbyqxmd.com/read/29324824/assessing-the-links-among-environmental-contaminants-endocrinology-and-parasites-to-understand-amphibian-declines-in-montane-regions-of-costa-rica
#10
Christopher J Leary, Hannah F Ralicki, David Laurencio, Sarah Crocker-Buta, John H Malone
Amphibians inhabiting montane riparian zones in the Neotropics are particularly vulnerable to decline, but the reasons are poorly understood. Because environmental contaminants, endocrine disruption, and pathogens often figure prominently in amphibian declines it is imperative that we understand how these factors are potentially interrelated to affect montane populations. One possibility is that increased precipitation associated with global warming promotes the deposition of contaminants in montane regions...
2018: PloS One
https://www.readbyqxmd.com/read/29323777/optimization-of-the-surface-modification-process-of-crosslinked-polythiol-coated-chiral-stationary-phases-synthesized-by-a-two-step-thiol-ene-click-reaction
#11
Kristina Schmitt, Michael Lämmerhofer
A new platform technology for the preparation of stable chiral stationary phases was successfully optimized. The chiral selector tert-butylcarbamoylquinine was firstly covalently connected to the polymer poly(3-mercaptopropyl)methylsiloxane by thiol-ene click reaction. Secondly, the quinine carbamate functionalized polysiloxane conjugate was coated onto the surface of vinyl modified silica particles and crosslinked via thiol-ene click reaction. The amount of polysiloxane, chiral selector, radical initiator, reaction solvent (chloroform and methanol), reaction time, and pore size of the supporting silica particles were varied and systematically optimized in terms of achievable plate numbers while maintaining simultaneously enantioselectivity...
January 11, 2018: Journal of Separation Science
https://www.readbyqxmd.com/read/29318096/a-two-photon-ratiometric-fluorescent-probe-for-imaging-of-hydrogen-peroxide-levels-in-rat-organ-tissues
#12
Chang Su Lim, Myoung Ki Cho, Mi Yeon Park, Hwan Myung Kim
Hydrogen peroxide (H2O2) is important in the regulation of a variety of biological processes and is involved in various diseases. Quantitative measurement of H2O2 levels at the subcellular level is important for understanding its positive and negative effects on biological processes. Herein, a two-photon ratiometric fluorescent probe (SHP-Cyto) with a boronate-based carbamate leaving group as the H2O2 reactive trigger and 6-(benzo[d]thiazol-2'-yl)-2-(N,N-dimethylamino) naphthalene (BTDAN) as the fluorophore was synthesized and examined for its ability to detect cytosolic H2O2 in situ...
January 2018: ChemistryOpen
https://www.readbyqxmd.com/read/29310704/mapping-insecticide-resistance-in-anopheles-gambiae-s-l-from-c%C3%A3-te-d-ivoire
#13
Soromane Camara, Alphonsine A Koffi, Ludovic P Ahoua Alou, Kouakou Koffi, Jean-Paul K Kabran, Aboubacar Koné, Mathieu F Koffi, Raphaël N'Guessan, Cédric Pennetier
BACKGROUND: Insecticide resistance in malaria vectors is an increasing threat to vector control tools currently deployed in endemic countries. Resistance management must be an integral part of National Malaria Control Programmes' (NMCPs) next strategic plans to alleviate the risk of control failure. This obviously will require a clear database on insecticide resistance to support the development of such a plan. The present work gathers original data on insecticide resistance between 2009 and 2015 across Côte d'Ivoire in West Africa...
January 8, 2018: Parasites & Vectors
https://www.readbyqxmd.com/read/29297804/suspected-carbaryl-toxicity-in-a-captive-colony-of-straw-colored-fruit-bats-eidolon-helvum
#14
Michael Selig, Albert Lewandowski
Carbaryl was the first carbamate insecticide produced and remains the most widely used due to its perceived low level of toxicity in nontarget species. This report describes the management and evaluation of a group of straw-colored fruit bats, Eidolon helvum, that were exposed to carbaryl. Cholinesterase activity of blood, retina, and brain was evaluated to further investigate whether carbaryl was the causative agent. Decreased whole blood and retinal cholinesterase activity coupled with the response to atropine suggests that the cause of the clinical signs in this bat colony was due to carbaryl exposure...
December 2017: Journal of Zoo and Wildlife Medicine: Official Publication of the American Association of Zoo Veterinarians
https://www.readbyqxmd.com/read/29295929/the-prodrug-of-7-8-dihydroxyflavone-development-and-therapeutic-efficacy-for-treating-alzheimer-s-disease
#15
Chun Chen, Zhihao Wang, Zhentao Zhang, Xia Liu, Seong Su Kang, Ying Zhang, Keqiang Ye
The BDNF mimetic compound 7,8-dihydroxyflavone (7,8-DHF), a potent small molecular TrkB agonist, displays prominent therapeutic efficacy against Alzheimer's disease (AD). However, 7,8-DHF has only modest oral bioavailability and a moderate pharmacokinetic (PK) profile. To alleviate these preclinical obstacles, we used a prodrug strategy for elevating 7,8-DHF oral bioavailability and brain exposure, and found that the optimal prodrug R13 has favorable properties and dose-dependently reverses the cognitive defects in an AD mouse model...
January 2, 2018: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/29291407/urine-volatile-organic-compounds-as-biomarkers-for-minimal-change-type-nephrotic-syndrome
#16
Desheng Liu, Nana Zhao, Mingao Wang, Xin Pi, Yue Feng, Yue Wang, Hongshuang Tong, Lin Zhu, Changsong Wang, Enyou Li
Urinary volatile organic compounds (VOCs) profiling has recently received considerable attention because it can be obtained noninvasively and conveniently while it can be successfully used in a variety of diseases and can provide unique biomarkers. The aim of current study was to investigate potential biomarkers between minimal change type nephrotic syndrome (MCNS) and normal. Urinary samples were collected from 38 minimal change type nephrotic syndrome patients and 15 healthy controls. Solid phase microextraction (SPME) and chromatography- mass spectrometry (GC-MS) were used to analysis the urinary metabolites...
December 29, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29288939/synthesis-and-anticancer-activity-of-novel-water-soluble-benzimidazole-carbamates
#17
Jae Eun Cheong, Michela Zaffagni, Ivy Chung, Yingjie Xu, Yiqiang Wang, Finith E Jernigan, Bruce R Zetter, Lijun Sun
Metastases account for more than 90% of all cancer deaths and respond poorly to most therapies. There remains an urgent need for new therapeutic modalities for the treatment of advanced metastatic cancers. The benzimidazole methylcarbamate drugs, commonly used as anti-helmitics, have been suggested to have anticancer activity, but progress has been stalled by their poor water solubility and poor suitability for systemic delivery to disseminated cancers. We synthesized and characterized the anticancer activity of novel benzimidazoles containing an oxetane or an amine group to enhance solubility...
December 14, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29279275/a-convenient-transesterification-method-for-synthesis-of-at2-receptor-ligands-with-improved-stability-in-human-liver-microsomes
#18
Johan Wannberg, Rebecka Isaksson, Ulf Bremberg, Maria Backlund, Jonas Sävmarker, Mathias Hallberg, Mats Larhed
A series of AT2R ligands have been synthesized applying a quick, simple, and safe transesterification-type reaction whereby the sulfonyl carbamate alkyl tail of the selective AT2R antagonist C38 was varied. Furthermore, a limited number of compounds where acyl sulfonamides and sulfonyl ureas served as carboxylic acid bioisosteres were synthesized and evaluated. By reducing the size of the alkyl chain of the sulfonyl carbamates, ligands 7a and 7b were identified with significantly improved in vitro metabolic stability in both human and mouse liver microsomes as compared to C38 while retaining the AT2R binding affinity and AT2R/AT1R selectivity...
November 24, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29274435/dietary-cumulative-acute-risk-assessment-of-organophosphorus-carbamates-and-pyrethroids-insecticides-for-the-brazilian-population
#19
Andreia Nunes Oliveira Jardim, Alessandra Page Brito, Gerda van Donkersgoed, Polly E Boon, Eloisa Dutra Caldas
Cumulative acute dietary risk assessments of organophosphorus (OPs), carbamates (CBs) and pyrethroids (PYs) were conducted for the Brazilian population. Residue data for 30786 samples of 30 foods were obtained from two national monitoring programs and one University laboratory, and consumption data from a national survey conducted among persons 10 years or older. Acephate and methamidophos were used as index compounds (IC) for OPs, oxamyl for CBs and deltamethrin for PYs. Exposures were estimated using the Monte Carlo Risk Assessment (MCRA 8...
December 20, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/29259666/rh-ii-mediated-domino-4-1-annulation-of-%C3%AE-cyanothioacetamides-using-diazoesters-a-new-entry-for-the-synthesis-of-multisubstituted-thiophenes
#20
Jury J Medvedev, Ilya V Efimov, Yuri M Shafran, Vitaliy V Suslonov, Vasiliy A Bakulev, Valerij A Nikolaev
A new approach towards the synthesis of multisubstituted thiophenes is elaborated based on Rh(II)-catalyzed domino reactions of acyclic diazoesters with α-cyanothioacetamides. It provides a way for the preparation of 5-amino-3-(alkoxycarbonylamino)thiophene-2-carboxylates, 2-(5-amino-2-methoxycarbonylthiophene-3-yl)aminomalonates and (2-cyano-5-aminothiophene-3-yl)carbamates with the preparative yields of up to 67%. It was also shown that α-cyanothioacetamides easily interact with dirhodium carboxylates to give rather stable 2:1 complexes, resulting in an evident decrease in the efficiency of the catalytic process at moderate temperatures (20-30 °C)...
2017: Beilstein Journal of Organic Chemistry
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