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Stephan Sinn, Frank Biedermann, Luisa De Cola
A reactive phosphorescent probe for aza-heterocyclic drugs and toxins was developed, affording a supramolecular emission-switch-on chemosensor in water. Complex formation of the heterocycles with a platinum(II) precursor proceeds readily at ambient conditions, allowing for facile analyte screening. 52 structurally diverse compounds were tested, out of which 23 pyridines, imidazole, and triazoles formed strongly emissive complex aggregates. Importantly, they all can be clearly distinguished from each other through a principal component analysis, but often already by simple visual inspection, e...
December 1, 2016: Chemistry: a European Journal
K M Sharnabai, M Krishnamurthy, N R Sagar, L Santhosh, Sureshbabu V Vommina
An efficient oxidative chlorination of thiols to Nα-protected amino alkyl sulfonyl azides is delineated. The reaction involves in situ generation of sulfonyl chloride employing N-chlorosuccinimide and tetrabutylammonium chloride-water in acetonitrile, followed by the reaction with sodium azide. The protocol is simple, straight forward, mild and high yielding. Amino acids with simple as well as bifunctional side chains were used to obtain Nα-protected amino alkyl sulfonyl azides. Further, sulfonyl azides were utilized to synthesize unnatural amino acids via Cu(OAc)2...
November 30, 2016: Protein and Peptide Letters
Joel D A Tyndall, Manya Sabherwal, Alia A Sagatova, Mikhail V Keniya, Jacopo Negroni, Rajni K Wilson, Matthew A Woods, Klaus Tietjen, Brian C Monk
Azole antifungals, known as demethylase inhibitors (DMIs), target sterol 14α-demethylase (CYP51) in the ergosterol biosynthetic pathway of fungal pathogens of both plants and humans. DMIs remain the treatment of choice in crop protection against a wide range of fungal phytopathogens that have the potential to reduce crop yields and threaten food security. We used a yeast membrane protein expression system to overexpress recombinant hexahistidine-tagged S. cerevisiae lanosterol 14α-demethylase and the Y140F or Y140H mutants of this enzyme as surrogates in order characterize interactions with DMIs...
2016: PloS One
Marek Łukasz Roszko, Marta Kamińska, Krystyna Szymczyk, Renata Jędrzejczak
Chemical plant protection is a commonly discussed factor potentially responsible for decline in pollinators and other beneficial insect populations. Various groups of chemicals including persistent organic pollutants could impact a bee colony's welfare and are reported to be present in bee tissue and apiary products. The aim of this work was to evaluate the presence of selected persistent organic pollutant and pesticide residues in bee pollen originating from different geographical regions of Poland. Pesticide residues were identified in 60% of tested bee pollen samples...
2016: PloS One
C P Kaushik, Raj Luxmi, Dharmendra Singh, Ashwani Kumar
Twenty ester-linked 1,4-disubstituted 1,2,3-triazoles having a furyl/thienyl moiety have been synthesized from heteroaryl prop-2-yn-1-yl carboxylate and aromatic azides via a Cu(I) catalyzed 1,3-dipolar cycloaddition. All the synthesized compounds were characterized by FTIR, [Formula: see text]H NMR, [Formula: see text]C NMR spectroscopy and HRMS. Synthesized triazoles were tested in vitro for antimicrobial evaluation against Gram-negative bacteria-Escherichia coli, Enterobacter aerogenes and Klebsiella pneumoniae; Gram-positive bacteria-Staphylococcus aureus and two fungal strains-Candida albicans and Aspergillus niger, reflecting moderate to good activity...
November 29, 2016: Molecular Diversity
Tarsis F Brust, Jenny Morgenweck, Susy A Kim, Jamie H Rose, Jason L Locke, Cullen L Schmid, Lei Zhou, Edward L Stahl, Michael D Cameron, Sarah M Scarry, Jeffrey Aubé, Sara R Jones, Thomas J Martin, Laura M Bohn
Agonists targeting the kappa opioid receptor (KOR) have been promising therapeutic candidates because of their efficacy for treating intractable itch and relieving pain. Unlike typical opioid narcotics, KOR agonists do not produce euphoria or lead to respiratory suppression or overdose. However, they do produce dysphoria and sedation, side effects that have precluded their clinical development as therapeutics. KOR signaling can be fine-tuned to preferentially activate certain pathways over others, such that agonists can bias signaling so that the receptor signals through G proteins rather than other effectors such as βarrestin2...
November 29, 2016: Science Signaling
Alejandra Huete-Soto, Mario Masís-Mora, Verónica Lizano-Fallas, Juan Salvador Chin-Pampillo, Elizabeth Carazo-Rojas, Carlos E Rodríguez-Rodríguez
The biopurification systems (BPS) used for the treatment of pesticide-containing wastewater must present a versatile degrading ability, in order to remove different active ingredients according to the crop protection programs. This work aimed to assay the simultaneous removal of several pesticides (combinations of herbicides/insecticides/fungicides, or insecticides/fungicides) in a biomixture used in a BPS over a period of 115 d, and in the presence of oxytetracycline (OTC), an antibiotic of agricultural use that could be present in wastewater from agricultural pesticide application practices...
November 26, 2016: Chemosphere
María Victoria Castelli, Marcos Gabriel Derita, Silvia Noelí López
Superficial infections involving the skin and mucosa are the most common fungal disease in humans. Fungi can also produce invasive infections (IFI), which are increasing in incidence among the growing population of immunocompromised patients, and are characterized by a high mortality rate. Amphotericin B, new triazoles and echinocandins have improved treatment options in IFI. However, the frequency of less common and more resistant fungi, the limited activity of available antifungal drugs and their undesirable side effects reflect the urgent need for the development of new therapeutic strategies...
November 29, 2016: Expert Opinion on Therapeutic Patents
Zhao-Xi Wang, Lin-Fei Wu, Xuan Zhang, Feifei Xing, Ming-Xing Li
Six novel Co(ii) coordination polymers, namely, [Co10L6(OH)2(H2O)9]·10.5H2O (1), [Co3L2(3-abpt)2]·4H2O (2), [Co3L2(4-azpy)2(H2O)2(EtOH)] (3), [Co3L2(4,4'-bipy)2(H2O)2(MeCN)] (4), [Co3L2(4,4'-bipy)2] (5), and [Co5L2(OH)2(ina)2(H2O)2] (6) (H3L = 2,2'-phosphinico-dibenzoic acid, 3-abpt = 4-amino-3,5-bis(3-pyridyl)-1,2,4-triazole, 4-azpy = 4,4'-azobispyridine, 4,4'-bipy = 4,4'-bipyridine, Hina = isonicotinic acid), have been hydrothermally synthesized and their magnetic properties have been characterized. The L(3-) anion displays six types of coordination modes in the compounds...
November 29, 2016: Dalton Transactions: An International Journal of Inorganic Chemistry
Si-Yang Liu, Dong-Dong Zhou, Chun-Ting He, Pei-Qin Liao, Xiao-Ning Cheng, Yan-Tong Xu, Jia-Wen Ye, Jie-Peng Zhang, Xiao-Ming Chen
Mixing molecular building blocks in the solid solution manner is a valuable strategy to obtain structures and properties in between the isostructural parent metal-organic frameworks (MOFs). We report nonlinear/synergistic solid-solution effects using highly related yet non-isostructural, phosphorescent Cu(I) triazolate frameworks as parent phases. Near the phase boundaries associated with conformational diversity and ligand heterogeneity, the porosity (+150 %) and optical O2 sensitivity (410 times, limit of detection 0...
November 28, 2016: Angewandte Chemie
D V Korabel'nikov, Yu N Zhuravlev
The structural and electronic properties of energetic nitrates with organic cations (uronium and 3,3'-diamino-4,4'-azo-1,2,4-triazole) and a metal-organic framework crystal [Ag(ethylenediamine)]NO3 have been investigated using density functional theory including van der Waals interactions. It is found that the linear compressibility of urea nitrate is positive and anisotropic (a ≈ b < c), whereas 3,3'-diamino-4,4'-azo-1,2,4-triazole nitrate and [Ag(ethylenediamine)]NO3 show both positive and negative linear compressibility along the b, c and a-axes, respectively...
November 25, 2016: Physical Chemistry Chemical Physics: PCCP
Vlastimil Mazanek, Alena Libanska, Jiri Sturala, Daniel Bouša, David Sedmidubský, Martin Pumera, Zbynek Janousek, Jan Plutnar, Zdenek Sofer
Fluorographene is the youngest stoichiometric derivative of graphene, thus, its reactivity is just poorly explored. Compared to graphene, a significantly higher reactivity of C-F bonds makes this material a suitable platform for a large number of chemical modifications. Fluorographene is also the only member of halogengraphenes family, which can be prepared in stoichiometric composition C1F1. Here, we present the chemical modification of fluorographene with Grignard reagents which are well known in organic chemistry for the formation of new C-C bonds...
November 23, 2016: Chemistry: a European Journal
Daniel Mendoza-Espinosa, David Rendón-Nava, Alejandro Alvarez-Hernández, Deyanira Angeles-Beltrán, Guillermo Enrique Negrón-Silva, Oscar Rodolfo Suárez-Castillo
Reaction of triazolium precursors [MIC(CH2)n-H+]I- (n = 1-3) with potassium hexamethyldisilazane (KHMDS) and AuCl(SMe2) generates the gold(I) complexes of the type MIC(CH2)n*AuI. Visible light exposure of the latter complexes promotes a spontaneous disproportionation process rendering gold(III) complexes of the type [{MIC(CH2)n}2*AuI2]+I-. Both the Au(I) and Au(III) complex series were tested in the catalytic hydrohydrazination of terminal alkynes using hydrazine as nitrogen source.
November 23, 2016: Chemistry, An Asian Journal
Anca Stana, Alexandra Enache, Dan Cristian Vodnar, Cristina Nastasă, Daniela Benedec, Ioana Ionuț, Cezar Login, Gabriel Marc, Ovidiu Oniga, Brîndușa Tiperciuc
In the context of the dangerous phenomenon of fungal resistance to the available therapies, we present here the chemical synthesis of a new series of thiazolyl-triazole Schiff bases B1-B15, which were in vitro assessed for their anti-Candida potential. Compound B10 was found to be more potent against Candida spp. when compared with the reference drugs Fluconazole and Ketoconazole. A docking study of the newly synthesized Schiff bases was performed, and results showed good binding affinity in the active site of co-crystallized Itraconazole-lanosterol 14α-demethylase isolated from Saccharomyces cerevisiae...
November 22, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Lin You, Chengwei Zhang, Nageswari Yarravarapu, Lorraine Morlock, Xiaolei Wang, Lishu Zhang, Noelle S Williams, Lawrence Lum, Chuo Chen
The acyltransferase Porcupine (Porcn) is essential for the secretion of Wnt proteins which contribute to embryonic development, tissue regeneration, and tumorigenesis. We have previously discovered four molecular scaffolds harboring Porcn-inhibitory activity. Comparison of their structures led to the identification of a general scaffold that can be readily assembled by modular synthesis. We report herein the development of a triazole version of this new class of Porcn inhibitors. This study yielded IWP-O1, a Porcn inhibitor with an EC50 value of 80pM in a cultured cell reporter assay of Wnt signaling...
December 15, 2016: Bioorganic & Medicinal Chemistry Letters
Minjian Huang, Zixin Deng, Jian Tian, Tiangang Liu
Salinomycin, a polyether antibiotic used for treatment of coccidial disease in animal husbandry, has demonstrated promising efficacy for treating different cancers. To enrich structure-activity relationship of salinomycin in tumours, we prepared a series of new triazole derivatives in specific site of salinomycin by click cycloaddition reactions, and assessed their antiproliferative activities on breast cancer cell lines. The screening results indicated that most derivatives modified at the C20 hydroxyl group have potent antitumour activity...
November 2, 2016: European Journal of Medicinal Chemistry
Tomislav Gregorić, Mirela Sedić, Petra Grbčić, Andrea Tomljenović Paravić, Sandra Kraljević Pavelić, Mario Cetina, Robert Vianello, Silvana Raić-Malić
Regioselective 1,4-disubstituted 1,2,3-triazole tethered pyrimidine-2,4-dione derivatives (5-23) were successfully prepared by the copper(I)-catalyzed click chemistry. While known palladium/copper-cocatalyzed method based on Sonogashira cross-coupling followed by the intramolecular 5-endo-dig ring closure generated novel 6-alkylfuro[2,3-d]pyrimidine-2-one-1,2,3-triazole hybrids (24b-37b), a small library of their 5-alkylethynyl analogs (24a-37a) was synthesized and described for the first time by tandem terminal alkyne dimerization and subsequent 5-endo-trig cyclization, which was additionally corroborated with computational and X-ray crystal structure analyses...
November 14, 2016: European Journal of Medicinal Chemistry
Ian Strydom, Gregorio Guisado-Barrios, Israel Fernandez, David C Liles, Eduardo Peris, Daniela Ina Bezuidenhout
A series of novel cationic and neutral Rh-complexes with an N-donor functionalized 1,2,3-triazol-5-ylidene (TRZ) ligand (where pendant N-donor is NHBoc, NH2 or NMe2 respectively) is described. Their catalytic activity was evaluated towards the hydrothiolation of alkynes. Among the catalysts, a neutral dicarbonyl complex featuring the tethered-NBoc amido-TRZ ligand proved very selective for alkyne hydrothiolation with an aryl thiol. Remarkably, the reaction could be carried out in the absence of pyridine or base additive...
November 22, 2016: Chemistry: a European Journal
Bing Li, Yangyang Yu, Pengxiang Zhao, Shiyong Zhang
Featuring the advantages of both homogeneous (high activity) and heterogeneous (recyclability) catalysts, heterogenized homogeneous catalysts (e.g., dendrimer-stabilized metal nanoparticles) have received much attention in recent years. Here, we develop a new triazole-containing dendrimer-like core cross-linked micelle (DCCM) stabilized Pd nanoparticles as a highly efficient heterogenized homogeneous catalyst for the Suzuki-Miyaura reaction. Both arylboronic acids and iodobenzenes with diverse electronic properties performed with excellent reactivity under the mild conditions of room temperature, water as the sole solvent, and as low as 0...
November 22, 2016: Chemistry, An Asian Journal
Jun-Li Wang, Qiang Liu, Xiao-Jin Lv, Rui-Lin Wang, Chun-Ying Duan, Tao Liu
The rational design of magnetic and fluorescent bifunctional materials is attracting increasing interest. In this study, two mononuclear Fe(ii) complexes, namely [Fe(L)2(NCS)2] (1) and [Fe(L)2(NCSe)2] (2) are synthesised by combining a spin-crossover unit and a fluorescent ligand (naphth-1-yl)-N-(3,5-di(pyridin-2-yl)-4H-1,2,4-triazol-4-yl)methanimine (L) to achieve bifunctionality. Single-crystal X-ray studies and magnetic measurements confirm the presence of spin crossover behaviours; these measurements agree with the results of the temperature depended Raman spectra and infrared spectra...
November 22, 2016: Dalton Transactions: An International Journal of Inorganic Chemistry
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