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https://www.readbyqxmd.com/read/28319840/grafting-heteroelement-rich-groups-on-graphene-oxide-tuning-polarity-and-molecular-interaction-with-bio-ionic-liquid-for-enhanced-lubrication
#1
Liwen Mu, Yijun Shi, Xiaojing Guo, Wei Zhuang, Long Chen, Tuo Ji, Jing Hua, Huaiyuan Wang, Jiahua Zhu
Two different heteroelement-rich molecules have been successfully grafted on graphene oxide (GO) sheets which were then used as lubricant additives in bio-ionic liquid. The grafting was processed with reactions between GO sheets and synthesized heteroelement-rich molecules (Imidazol-1-yl phosphonic dichloride and 1H-1,2,4-triazol-1-yl phosphonic dichloride, respectively). The modified GO (m-GO) was added into [Choline][Proline] ([CH][P]) bio-ionic liquid, and has been demonstrated effective additive in promoting lubrication...
March 9, 2017: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/28319782/synthesis-and-antiplasmodial-activity-of-novel-indoleamide-derivatives-bearing-sulfonamide-and-triazole-pharmacophores
#2
N Devender, Sarika Gunjan, Renu Tripathi, Rama Pati Tripathi
Due to the recent reports of growing parasite resistance to artemisinins and other antimalarial drugs, development of new antimalarial chemotypes is an urgent priority. Here in, we report a novel series of adamantyl/cycloheptyl indoleamide derivatives bearing sulfonamide and triazole pharmacophores adopting different chemical modifications and evaluated them for antiplasmodial activity in vitro. Among all the indoleamides, compounds 22, 24, 26 and 30 with sulfonamide pharmacophore showed promising activity with IC50 of 1...
March 8, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28318747/ultra-fast-quantitation-of-voriconazole-in-human-plasma-by-coated-blade-spray-mass-spectrometry
#3
Marcos Tascon, Germán Augusto Gómez-Ríos, Nathaly Reyes-Garcés, Justen Poole, Ezel Boyacı, Janusz Pawliszyn
Voriconazole is a triazole broad-spectrum antifungal medication often used to treat fungal infections caused by Aspergillus and Fusarium species. One of the main challenges associated with the implementation of this medication is its narrow therapeutic concentration range, demonstrating toxicity at concentrations above 6μg/mL and limited efficacy at concentrations below 2μg/mL. As a result, methodologies which permit the rapid and accurate quantitation of voriconazole in patients are highly desirable. In this work two different approaches based on coated blade spray directly coupled to mass spectrometry (CBS-MS) are introduced; each enabling the quantitation of voriconazole in plasma samples with a simple and fast sample preparation and no chromatographic step...
March 12, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28315638/determination-of-triazines-and-triazoles-in-grapes-using-atmospheric-pressure-matrix-assisted-laser-desorption-ionization-high-resolution-mass-spectrometry
#4
Vishal Mahale, Ajeet Singh, Gayatri S Phadke, Avinash D Ghanate, Dasharath P Oulkar, Kaushik Banerjee, Venkateswarlu Panchagnula
A chromatography-free atmospheric pressure matrix-assisted laser desorption/ionization high-resolution mass spectrometry (AP-MALDI HRMS) method is described for the simultaneous and quantitative detection of triazines and triazoles in grapes. The analytes were detected reproducibly with high mass accuracy (mass error within 5 ppm) and further confirmed by collision-induced dissociation fragmentation in tandem MS. The LODs and LOQs for all the analytes were found to be in the nanogram per gram level (15-20 ng/g LOQ)...
March 18, 2017: Journal of AOAC International
https://www.readbyqxmd.com/read/28304029/convenient-preparation-of-4-diazoisochroman-3-imines-and-3-subsituted-3-5-dihydroisochromeno-3-4-d-1-2-3-triazoles
#5
Anni Ren, Ping Lu, Yanguang Wang
A novel and convenient preparation of 4-diazoisochroman-3-imines through the copper(i)-catalyzed cascade reaction of (2-ethynylphenyl)-methanols with sulfonyl azides is described. The synthesized cyclical α-diazo imidates could readily react with a variety of primary amines to furnish 3-substituted 3,5-dihydroisochromeno[3,4-d][1,2,3]-triazoles under catalyst-free conditions.
March 17, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/28303848/triazole-resistance-in-aspergillus-fumigatus-clinical-isolates-obtained-in-nanjing-china
#6
Ming Zhang, Chun-Lai Feng, Fei Chen, Qian He, Xin Su, Yi Shi
BACKGROUND: During the past decades, the incidence of invasive aspergillosis (IA) caused by Aspergillus fumigatus has increased dramatically. The aims of this study were to investigate the susceptibility of clinical isolates of A. fumigatus to triazole and the underlying cyp51A mutations in triazole-resistant A. fumigatus. METHODS: A total of 126 A. fumigatus clinical isolates from 126 patients with proven or probable IA were obtained from four large tertiary hospitals in Nanjing, China, between August 2012 and July 2015...
March 20, 2017: Chinese Medical Journal
https://www.readbyqxmd.com/read/28302510/bishomoisoprenoid-triazole-bisphosphonates-as-inhibitors-of-geranylgeranyl-diphosphate-synthase
#7
Veronica S Wills, Joseph I Metzger, Cheryl Allen, Michelle L Varney, David F Wiemer, Sarah A Holstein
Protein geranylgeranylation reactions are dependent on the availability of geranylgeranyl diphosphate (GGDP), which serves as the isoprenoid donor. Inhibition of GGDP synthase (GGDPS) is of interest from a drug development perspective as GGDPS inhibition results in impaired protein geranylgeranylation, which in multiple myeloma, disrupts monoclonal protein trafficking and induces apoptosis. We have recently reported a series of isoprenoid triazole bisphosphonates and have demonstrated that a 3:1 mixture of homogeranyl and homoneryl isomers potently, and in a synergistic manner, inhibits GGDPS...
March 4, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28301169/conformational-dynamics-of-cyanocobalamin-and-its-conjugates-with-peptide-nucleic-acids
#8
Tomasz Pieńko, Aleksandra J Wierzba, Monika Wojciechowska, Dorota Gryko, Joanna Trylska
Vitamin B12 also called cobalamin (Cbl) is an important enzymatic co-factor taken up by mammalian and also by many bacterial cells. Peptide nucleic acid (PNA) is a synthetic DNA analogue that has the ability to bind in a complementary manner to natural nucleic acids. Provided that PNA is efficiently delivered to cells, it could act as a steric blocker of functional DNA or RNA and regulate gene expression at the level of transcription or translation. Recently, Cbl has been examined as a transporter of various molecules to cells...
March 16, 2017: Journal of Physical Chemistry. B
https://www.readbyqxmd.com/read/28294601/gemini-type-tetraphenylethylene-amphiphiles-containing-12-anen3-and-long-hydrocarbon-chains-as-nonviral-gene-vectors-and-gene-delivery-monitors
#9
Ai-Xiang Ding, Zheng-Li Tan, You-Di Shi, Ling Song, Bing Gong, Zhong-Lin Lu
Four gemini amphiphiles decorated with triazole-[12]aneN3 as the hydrophilic moiety and various long-hydrocarbons as hydrophobic moieties, 1-4, were designed to form micelles possessing aggregation-induced emission (AIE) property for gene delivery and tracing. All four amphiphiles give ultralow critical micelle concentrations, are pH/photo-stable and biocompatible, and completely retard the migration of plasmid DNAs at low concentrations. The DNA-binding abilities of the micelles were fully assessed. The co-aggregated nanoparticles of 1‒4 with DNAs could convert back into AIE micelles...
March 15, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28293834/synthesis-and-evaluation-of-novel-hcv-replication-inhibitors
#10
David C McGowan, Mourad D Khamlichi, Alex De Groot, Frederik Pauwels, Frédéric Delouvroy, Kristof Van Emelen, Kenneth Simmen, Pierre Raboisson
Direct acting antiviral agents to cure hepatitis C virus (HCV) infection has emerged as the gold standard therapy. Along with protease inhibitors, nucleoside polymerase inhibitors and non-nucleoside polymerase inhibitors, the inhibition of NS5a has proved to be an effective way to treat HCV patients. Here we report on novel HCV NS5a inhibitors which were synthesized and evaluated in the HCV replicon assay. A series of inhibitors were formed by a cycloaddition reaction in parallel to establish new leads and explore the effects of unsymmetrical cap substitution...
March 14, 2017: Molecular Diversity
https://www.readbyqxmd.com/read/28290250/synthesis-and-ativiral-activity-of-5-benzylthio-4-carbamyl-1-2-3-triazoles-against-human-cytomegalovirus-cmv-and-varicella-zoster-virus-vzv
#11
Yi-Ning Wen, Zhi-Feng Zhang, Ning-Ning Liu, Graciela Andrei, Robert Snoeck, Yu-Hong Xiang, Dominique Schols, Xue Chen, Zhuo-Yong Zhang, Qing-Shan Zhang, Qin-Pei Wu
BACKGROUND: All of clinic drugs for herpesvirus infections exhibit high toxicity and suffer from significant drug-resistantance. There is a great need for the development of new, effective, and safe anti-herpesvirus agents with different mechanisms of action. METHODS: A series of novel 5-(benzylthio)-1H-1,2,3- triazole-4-carboxamides were efficiently synthesized and EC50 values against human cytomegalovirus (HCMV), varicella-zoster virus (VZV) and herpes simplex virus (HSV) were evaluated in vitro...
March 7, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28287716/biocide-runoff-from-building-facades-degradation-kinetics-in-soil
#12
Ulla Elisabeth Bollmann, David Fernández-Calviño, Kristian Koefoed Brandt, Morten Swayne Storgaard, Hans Sanderson, Kai Bester
Biocides are common additives in building materials. In-can and film preservatives in polymer-resin render and paint, as well as wood preservatives are used to protect facade materials from microbial spoilage. Biocides leach from the facade material with driving rain, leading to highly polluted runoff water (up to several mg L(-1) biocides) being infiltrated into the soil surrounding houses. In the present study the degradation rates in soil of eleven biocides used for the protection of building materials were determined in laboratory microcosms...
March 13, 2017: Environmental Science & Technology
https://www.readbyqxmd.com/read/28287569/self-assembling-morphologies-obtained-from-helical-polycarbodiimide-copolymers-and-their-triazole-derivatives
#13
Oleg V Kulikov, Dumindika A Siriwardane, Gregory T McCandless, Samsuddin F Mahmood, Bruce M Novak
A facile method for the preparation of polycarbodiimide-based secondary structures (e.g., nano-rings, "craters," fibers, looped fibers, fibrous networks, ribbons, worm-like aggregates, toroidal structures, and spherical particles) is described. These aggregates are morphologically influenced by extensive hydrophobic side chain-side chain interactions of the singular polycarbodiimide strands, as inferred by atomic force microscopy (AFM) and scanning electron microscopy (SEM) techniques. Polycarbodiimide-g-polystyrene copolymers (PS-PCDs) were prepared by a combination of synthetic methods, including coordination-insertion polymerization, copper(I)-catalyzed azide alkyne cycloaddition (CuAAC) "click" chemistry, and atom transfer radical polymerization (ATRP)...
February 7, 2017: Journal of Visualized Experiments: JoVE
https://www.readbyqxmd.com/read/28285876/one-pot-synthesis-of-a-new-2-substituted-1-2-3-triazole-1-oxide-derivative-from-dipyridyl-ketone-and-isonitrosoacetophenone-hydrazone-nickel-ii-complex-dna-binding-and-cleavage-properties
#14
Ramazan Gup, Oktay Erer, Nefise Dilek
An efficient and simple one-pot synthesis of a new 1,2,3-triazole-1-oxide via reaction between isonitrosoacetophenone hydrazone and dipyridyl ketone in the EtOH/AcOH at room temperature has been developed smoothly in high yield. The reaction proceeds via metal salt free, in-situ formation of asymmetric azine followed by cyclization to provide 1,2,3-triazole 1-oxide compound. It has been structurally characterized. The 1:1 ratio reaction of the 1,2,3-triazole 1-oxide ligand with nickel(II) chloride gives the mononuclear complex [Ni(L)(DMF)Cl2], hexa-coordinated within an octahedral geometry...
March 3, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28283969/the-key-role-of-biogenic-manganese-oxides-in-enhanced-removal-of-highly-recalcitrant-1-2-4-triazole-from-bio-treated-chemical-industrial-wastewater
#15
Ruiqin Wu, Haobo Wu, Xinbai Jiang, Jinyou Shen, Muhammad Faheem, Xiuyun Sun, Jiansheng Li, Weiqing Han, Lianjun Wang, Xiaodong Liu
The secondary effluent from biological treatment process in chemical industrial plant often contains refractory organic matter, which deserves to be further treated in order to meet the increasingly stringent environmental regulations. In this study, the key role of biogenic manganese oxides (BioMnOx) in enhanced removal of highly recalcitrant 1,2,4-triazole from bio-treated chemical industrial wastewater was investigated. BioMnOx production by acclimated manganese-oxidizing bacterium (MOB) consortium was confirmed through scanning electronic microscopy (SEM), X-ray photoelectron spectroscopy (XPS), and X-ray diffraction (XRD) analysis...
March 10, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28281720/n-1-selective-alkenylation-of-1-sulfonyl-1-2-3-triazoles-with-alkynes-via-gold-catalysis
#16
Chenyang Sun, Xiao Yuan, Yan Li, Xiaoxiao Li, Zhigang Zhao
A N(1)-selective alkenylation of 1-sulfonyl-1,2,3-triazoles with alkynes via gold catalysis is reported. N(1)-Vinyl substituted 1,2,3-triazoles were selectively prepared in up to 92% yield through the sulfonyl group of 1,2,3-triazole derivatives transformed to alkenyl groups in a "one-pot two steps" manner. This method provided a new method for the synthesis of potentially biological-active vinyl-triazole building blocks.
March 10, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28281345/singlet-versus-triplet-excited-state-mediated-photoin-duced-dehalogenation-reactions-of-itraconazole-in-acetonitrile-and-aqueous-solutions
#17
Ruixue Zhu, Ming-De Li, Lili Du, David Lee Phillips
The photoinduced dehalogenation of the antifungal drug Itraconazole in acetonitrile and acetonitrile/water mixed solutions was investigated using femtosecond and nanosecond time-resolved transient absorption (fs-TA and ns-TA) and nanosecond time-resolved resonance Raman spectroscopy (ns-TR3) experiments. An excited resonance energy transfer was found to take place from the 4-phenyl-4,5-dihydro-3H-1,2,4-triazol-3-one part of the molecule to the 1,3-dichlorobenzene part of the molecule when Itraconazole is excited by ultraviolet light...
March 10, 2017: Journal of Physical Chemistry. B
https://www.readbyqxmd.com/read/28275772/rapidly-accessible-click-rotaxanes-utilizing-a-single-amide-hydrogen-bond-templating-motif
#18
Beth E Fletcher, Michael J G Peach, Nicholas H Evans
The synthesis of hydrogen bond templated rotaxanes using the CuAAC click reaction has been achieved in yields of up to 47%, employing near stoichiometric equivalents of macrocycle and readily prepared azide and alkyne half-axle components. Interlocked structure formation has been confirmed by NMR spectroscopy and mass spectrometry. Density functional theory calculations support (1)H NMR spectroscopic analysis that the macrocycle resides over the amide of the axle component, rather than the newly formed triazole, as a result of more favourable hydrogen bond interactions...
March 9, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28273562/identification-of-dibenzyl-imidazolidine-and-triazole-acetamide-derivatives-through-virtual-screening-targeting-amyloid-beta-aggregation-and-neurotoxicity-in-pc12%C3%A2-cells
#19
Sukanya Das, Scott D Smid
Aggregation and neurotoxicity of amyloid β (Aβ) protein is a hallmark characteristic of Alzheimer's disease (AD). In this study we compared the anti-aggregatory and neuroprotective effects of five synthetic compounds against Aβ protein; four of which possessed a five membered heterocycle ring scaffold (two dibenzyl phenyl imidazolidines and two triazole sulfanyl acetamides) and one with a fused five membered heterocycle (benzoxazole) ring, selected thorough virtual screening from ZINC database. Molecular docking of their optimized structures was used to study Aβ binding characteristics...
April 21, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28272894/1-4-substituted-triazoles-as-nonsteroidal-anti-androgens-for-prostate-cancer-treatment
#20
Claudia Ferroni, Antonella Pepe, Yeong Sang Kim, Sunmin Lee, Andrea Guerrini, Marco Daniele Parenti, Anna Tesei, Alice Zamagni, Michela Cortesi, Nadia Zaffaroni, Michelandrea De Cesare, Giovanni Luca Beretta, Jane B Trepel, Sanjay V Malhotra, Greta Varchi
Prostate cancer (PC) is the fifth leading cause of cancer death in men, and the androgen receptor (AR) represents the primary target for PC treatment, even though the disease frequently progresses toward androgen-independent forms. Most of the commercially available nonsteroidal antiandrogens show a common scaffold consisting of two aromatic rings connected by a linear or a cyclic spacer. By taking advantage of a facile, one-pot click chemistry reaction, we report herein the preparation of a small library of novel 1,4-substituted triazoles with AR antagonistic activity...
March 20, 2017: Journal of Medicinal Chemistry
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