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Lambros Messinis, Dimitris Apostolopoulos, Tryfon Spiridonidis, Grigorios Nasios, Aikaterini Giazkoulidou, Magda Tsolaki, Vasilis Panagiotopoulos
OBJECTIVES: Cognitive impairment is present in up to 65% of Relapsing Remitting Multiple sclerosis (RRMS) patients and can be extremely debilitating. Although deficits in episodic memory and processing speed occur more frequently than executive deficits, executive dysfunction tends to have a significant impact on MS patients' ability to generate strategies, think divergently, solve and estimate problems, and reason in abstract terms with substantial negative impacts on activities of daily living...
January 2019: Hellenic Journal of Nuclear Medicine
Wei Li, Xiujuan Xu, Baoling Lyu, Ying Tang, Yinlong Zhang, Fang Chen, Gregory Korshin
The degradation of roxithromycin (ROX) by hydroxyl radical (·OH) generated by UV/H2 O2 was systematically investigated in terms of degradation kinetics, effects of water chemistry parameters, oxidation products, as well as toxicity evaluation. The degradation of ROX by UV/H2 O2 with varying light irradiation intensity, initial ROX concentration, and H2 O2 concentration in pure water and wastewater all followed pseudo-first-order kinetics. The second-order rate constant for reaction between ROX and ·OH is 5...
March 14, 2019: Environmental Science and Pollution Research International
Katherine McReynolds, Dustin Dimas, Grace Floyd, Kara Zeman
A rapid, high-yielding microwave-mediated synthetic procedure was developed and optimized using a model system of monovalent sugar linkers, with the ultimate goal of using this method for the synthesis of multivalent glycoclusters. The reaction occurs between the aldehyde/ketone on the sugars and an aminooxy moiety on the linker/trivalent core molecules used in this study, yielding acid-stable oxime linkages in the products and was carried out using equimolar quantities of reactants under mild aqueous conditions...
March 14, 2019: Pharmaceuticals
Peiqi Zhou, Yubing Huang, Wanqing Wu, Wentao Yu, Jianxiao Li, Zhongzhi Zhu, Huanfeng Jiang
A novel strategy for constructing sulfur containing bis-S-heterocyclic compounds from oxime esters/vinyl azide, phenylacetylene/aldehydes and elemental sulfur (S8) has been developed. These transformations show good functional group tolerance. Various bis-S-heterocyclic products were efficiently synthesized from easily prepared or widely commercially available starting materials. In this protocol, S8 successfully served as a two-sulfur atom donor for thiophene and thiazole rings, respectively.
March 14, 2019: Organic & Biomolecular Chemistry
Niko Amend, Horst Thiermann, Franz Worek, Timo Wille
The global use of organophosphorus compounds (OP) for pest control and nerve agents being used in military conflicts and for assassinations renders intoxications by these agents a public health concern. OP-poisoned patients often suffer from dysrhythmias which may ultimately result in death. In this study, human-induced pluripotent stem cells derived cardiomyocytes were exposed to OP compounds in a microelectrode array system (MEA). The MEA system is widely accepted to assess the proarrhythmic properties of (candidate) drugs...
March 8, 2019: Toxicology Letters
Noëmie Jean LeBlanc, Romain Menet, Katherine Picard, Geneviève Parent, Marie-Ève Tremblay, Ayman ElAli
Stroke induces blood-brain barrier (BBB) breakdown, which promotes complications like oedema and hemorrhagic transformation. Administration of recombinant tissue plasminogen activator (rtPA) within a therapeutic time window of 4.5 h after stroke onset constitutes the only existing treatment. Beyond this time window, rtPA worsens BBB breakdown. Canonical Wnt pathway induces BBB formation and maturation during ontogeny. We hypothesized that the pathway is required to maintain BBB functions after stroke; thus, its activation might improve rtPA therapy...
March 9, 2019: Molecular Neurobiology
Cong-Xuan Ma, Wei Lv, Ya-Xin Li, Bing-Zhi Fan, Xu Han, Fan-Sheng Kong, Jing-Chao Tian, Mark Cushman, Jian-Hua Liang
Constitutively erythromycin-resistant apathogens are more difficult to address than inducibly resistant and efflux-resistant strains. Three series of the 4th generation 2-fluoro 9-oxime erythromycin ketolides were synthesized and evaluated. Incorporation of substituted heteroaryl groups (a - m), in contrast to previously reported the unsubstituted heteroaryl groups, proved to the beneficial for enhancement of the activities of the 9-propgargyl ketolide 8 series and the 9-allyl ketolide 14 series. But these aryl groups (a - m) cannot supply the resulting compounds 8 and 14, unlike corresponding the 6-allyl ketolide 20 series, with activity against constitutively resistant Streptococcus pneumoniae...
March 3, 2019: European Journal of Medicinal Chemistry
Christina N Banti, Sotiris K Hadjikakou, Tuba Sismanoglu, Nick Hadjiliadis
Organotins(IV) exhibit significant in vitro anti-proliferative activity, while the in vivo tests are encouraging. The recent reports on the anti-proliferative activity of organotin(IV) compounds are summarized in this review. The period covered by this work goes back to 2009 until late 2018, while the earlier ones, are included over the previous review of our group published by S.K. Hadjikakou, N. Hadjiliadis, in Coord Chem Rev, 253 (2009) 235-249. During the last decade (2009-2018), >300 organotin(IV) derivatives with oxygen-donor ligands, such as carboxylic acids, amino-acids, Non Steroidal Anti-inflammatory Drugs (NSAIDs), biological active derivatives or natural products, organotins(IV) with sulfur containing ligands such as thiones, thiosemicarbazones, dithiocarbamates, organotin(IV) compounds of oximes and organotins(IV) with amines or semicarbazones were screened for their anti-proliferative effect against various cancer cell lines and their results are included in numerous reports over this period...
February 13, 2019: Journal of Inorganic Biochemistry
Grigory S Filonov, Wenjiao Song, Samie R Jaffrey
Fluorogenic aptamers are genetically encoded RNA aptamers that bind and induce the fluorescence of otherwise nonfluorescent small molecule dyes. These RNA-fluorophore complexes can be highly fluorescent and useful for RNA visualization and genetically encoded biosensors. Notably, different RNA aptamers can bind the same fluorophore resulting in complexes that exhibit spectrally distinct fluorescence properties. The basis for spectral tuning of small molecule fluorophores has not yet been studied. Here we explore the mechanism of spectral tuning in three highly related RNA aptamers, Broccoli, Orange Broccoli, and Red Broccoli, each of which binds the DFHO (3,5-difluoro-4-hydroxybenzylidene imidazolinone-2-oxime) fluorophore, and generates distinct spectral emissions...
March 6, 2019: Biochemistry
Adnan Hodžić, Albert Payer, Georg Gerhard Duscher
Over the last 30 years, Thelazia callipaeda (Spirurida: Thelaziidae) has increasingly been reported as an agent of ocular infections in animals and humans throughout Europe. Following the cases of canine ocular thelaziosis recently recorded in Austria for the first time, in the present paper, we describe the first case of T. callipaeda infection in an Austrian cat with no history of traveling abroad. This finding further supports the occurrence of the parasite's autochthonous transmission cycle in the country...
March 2, 2019: Parasitology Research
Sheemona Chowdhary, Rajasri Bhattacharyya, Dibyajyoti Banerjee
Acetylcholinesterase (AChE) is the primary target of organophosphorus pesticides (OPs). Ellman's method using Acetylthiocholine (ATCh) is the standard approach for the detection of AChE activity. Though ATCh is a popular substrate, it has certain drawbacks as well. Because of these limitations, there is a need for the development of reliable and rapid assays for determination of AChE activity in cases of OP poisoning. In the present work, we have used 1-Naphthyl acetate (1-NA) as a fluorogenic substrate for the estimation of AChE activity of human erythrocytes...
February 26, 2019: Biochimie
Wenyan Wang, Qingfei Song, Qing Liu, Hua Zheng, Chunmei Li, Yi Yan, Qiuyu Zhang
The covalent cross-linked rubber has outstanding mechanical properties and chemical resistance, making it possible for a wide range of applications. Towards efforts to resource waste and environmental pollution, rubber recycling is a concerning problem. However, it is a big challenge to endow the most widely used commercial rubber systems with recyclability. In this paper, a novel reprocessable and recyclable acrylonitrile-butadiene rubber (NBR) is developed by introducing oxime-carbamate bonds into the raw NBR...
February 28, 2019: Macromolecular Rapid Communications
Lu-Lu Chen, Jing-Wen Zhang, Wan-Wan Yang, Pei Chen, Dan-Yun Chen, Yan-Bo Wang
An effective and facile transition-metal-free method has been developed for the synthesis of β-ketophosphine oxides from alkynylphosphine oxides with benzaldehyde oxime as a hydroxide surrogate. The current methodology provides simple access to various β-ketophosphine oxides in moderate to excellent yields with a broad substrate scope.
February 28, 2019: Organic & Biomolecular Chemistry
Cody R Drisko, Silas A Griffin, Kevin S Huang
A convenient synthetic route for spirocyclic heterocycles is well sought after due to the molecule's potential use in biological systems. By means of solid-phase synthesis, regenerating Michael (REM) linker strategies, and 1,3-dipolar cycloaddition, a library of structurally similar heterocycles, both with and without a spirocyclic center, can be constructed. The main advantages of the solid-support synthesis are as follows: first, each reaction step can be driven to completion using a large excess of reagents resulting in high yields; next, the use of commercially available starting materials and reagents keep the costs low; finally, the reaction steps are easy to purify via simple filtration...
February 6, 2019: Journal of Visualized Experiments: JoVE
Reyna Zeferino-Díaz, Leticia Olivera-Castillo, Alberto Dávalos, George Grant, Nuvia Kantún-Moreno, Rossanna Rodriguez-Canul, Sylvain Bernès, Jesús Sandoval-Ramírez, María A Fernández-Herrera
22-Oxocholestanes bearing the oxime functionality in the side chain have been synthesized from diosgenin and evaluated in vivo as anti-inflammatory agents in an acute inflammation mouse ear model, against the commercial glucocorticoid dexamethasone. The final compounds were all regioselectively obtained with an E configuration at the oxime double bond. The title compounds reduced ear-induced inflammation and edema. The most active oximes repressed the expression of proinflammatory genes TNF-α, COX-2, and IL-6; including macrophage migration inhibitory factor...
February 13, 2019: European Journal of Medicinal Chemistry
Chloe Nguyen, Wei Ling Koh, Andrea Casteriano, Niek Beijerink, Christopher Godfrey, Graeme Brown, David Emery, Jan Šlapeta
Since publication of the original version of this article [1], it has been flagged that unfortunately there is an error in dosage units in the Discussion section, in the sentence "For example a microfilaricide, either ivermectin (50-200 mg/kg) or milbemycin oxime (500-1,000 mg/kg)".
February 19, 2019: Parasites & Vectors
Felix Kern, Klaus T Wanner
Generation and screening of oxime libraries by competitive MS Binding Assays represents a powerful tool for the identification of new compounds, with affinity to mGAT1, the most abundant plasma membrane bound GABA transporter in the CNS. By screening a guvacine derived oxime library, new potent inhibitors of mGAT1 had been revealed. In the present study, oxime libraries generated by reaction of a large excess of a rac-nipecotic acid derivative displaying a hydroxylamine functionality in which various aldehydes under suitable conditions, were examined for new potent inhibitors of mGAT1...
February 8, 2019: Bioorganic & Medicinal Chemistry
Chao Chang, Lei Han, Yanfang Zhao, Feng Li
Furfural content is considered as index to estimate transformer remnant life. Therefore, low cost, highly sensitive methods for determination of furfural are highly desirable. In the present work, we describe a new strategy for furfural detection by tracing the "off-on" fluorescence signals of fluorescent organic nanoparticles (FONPs). Significant H+ -dependent emission characteristics in aprotic organic solvent was found for our synthesized poly(DOPA)-FONPs. The fluorescence of poly(DOPA)-FONPs can be quickly quenched by hydroxylamine hydrochloride...
May 15, 2019: Talanta
Joanna Kozłowska, Ewa Grela, Dagmara Baczyńska, Agnieszka Grabowiecka, Mirosław Anioł
In our investigation, we concentrated on naringenin ( NG )-a widely studied flavanone that occurs in citrus fruits. As a result of a reaction with a range of alkyl iodides, 7 novel O -alkyl derivatives of naringenin ( 7a ⁻ 11a , 13a , 17a ) were obtained. Another chemical modification led to 9 oximes of O -alkyl naringenin derivatives ( 7b ⁻ 13b , 16b ⁻ 17b ) that were never described before. The obtained compounds were evaluated for their potential antibacterial activity against Escherichia coli , Staphylococcus aureus , and Bacillus subtilis ...
February 14, 2019: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Hong Dai, Meiling Huang, Jianqiang Qian, Ji Liu, Chi Meng, Yangyang Li, Guxu Ming, Ting Zhang, Senling Wang, Yujun Shi, Yong Yao, Shushan Ge, Yanan Zhang, Yong Ling
A series of hybrids 10a-v based on coumarin/pyrazole oxime have been synthesized, and exhibit good to excellent antitumor activities. Compound 10n has shown remarkable anticancer effect on SMMC-7721 cells (IC50  = 2.08 μM), which is considerably lower than 5-FU (IC50  = 37.8 μM) and similar to ADM (IC50  = 2.67 μM), with little effect on normal hepatic cells LO2. Notably, the suppression experiments of metastatic activities reveal that 10n also displays significant anti-metastasis effects through inhibiting cell migration and invasion in highly metastatic SMMC-7721 cell line, and dose-dependently reverses TGF-β1-induced epithelial-mesenchymal transition (EMT) procedure better than ADM...
January 30, 2019: European Journal of Medicinal Chemistry
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