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https://www.readbyqxmd.com/read/28432496/reproductive-effects-of-life-cycle-exposure-to-difenoconazole-on-female-marine-medaka-oryzias-melastigma
#1
Xiaocui Dong, Zhenghong Zuo, Jiaojiao Guo, Hongbin Li, Lemeng Zhang, Meng Chen, Zhibin Yang, Chonggang Wang
Difenoconazole (DFZ) is a widely used triazole fungicide which has been detected in some estuaries and embayments. This study was conducted to investigate the effects of DFZ on ovarian development in female marine medaka (Oryzias melastigma). After 180 days exposure of the embryo to DFZ (0, 1, 10, 100 and 1000 ng/L), the gonadosomatic index and percentage of mature oocytes produced were significantly reduced in the 1, 10 and 100 ng/L treatments but not the 1000 ng/L treatment compared to the control, thus exhibiting a U-shaped dose response curve...
April 21, 2017: Ecotoxicology
https://www.readbyqxmd.com/read/28430797/effect-of-quinoline-based-1-2-3-triazole-and-its-structural-analogues-on-growth-and-virulence-attributes-of-candida-albicans
#2
Mohammad Irfan, Shadab Alam, Nikhat Manzoor, Mohammad Abid
Candida albicans, along with some other non-albicans Candida species, is a group of yeast, which causes serious infections in humans that can be both systemic and superficial. Despite the fact that extensive efforts have been put into the discovery of novel antifungal agents, the frequency of these fungal infections has increased drastically worldwide. In our quest for the discovery of novel antifungal compounds, we had previously synthesized and screened quinoline containing 1,2,3-triazole (3a) as a potent Candida spp inhibitor...
2017: PloS One
https://www.readbyqxmd.com/read/28430422/gauging-donor-acceptor-properties-and-redox-stability-of-chelating-click-derived-triazoles-and-triazolylidenes-a-case-study-with-rhenium-i-complexes
#3
Lisa Suntrup, Sinja Klenk, Johannes Klein, Sebastian Sobottka, Biprajit Sarkar
Bidentate ligands containing at least one triazole or triazolylidene (mesoionic carbene, MIC) unit are extremely popular in contemporary chemistry. One reason for their popularity is the similarities as well as differences in the donor/acceptor properties that these ligands display in comparison to their pyridine or other N-heterocyclic carbene counterparts. We present here seven rhenium(I) carbonyl complexes where the bidentate ligands contain combinations of pyridine/triazole/triazolylidene. These are the first examples of rhenium(I) complexes with bidentate 1,2,3-triazol-5-ylidene-containing ligands...
April 21, 2017: Inorganic Chemistry
https://www.readbyqxmd.com/read/28429026/n-difluoromethyl-triazole-as-a-constrained-scaffold-in-peptidomimetics
#4
M Mamone, R S B Gonçalves, F Blanchard, G Bernadat, S Ongeri, T Milcent, B Crousse
The N-difluoromethyl triazolo-β-aza-ε-amino acid present in the core of peptides led to constrained conformations due to CH-F and NH-F interactions. Pseudotetrapeptides were obtained in excellent yields directly by click chemistry between azidodifluoroacetamides and alkynes, both linked to an amino acid. This work demonstrates that the N-difluoromethyltriazole scaffold can induce extended structures to β-strand mimics.
April 21, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/28426808/a-screen-for-protective-drugs-against-delayed-hypoxic-injury
#5
Chun-Ling Sun, Huiliang Zhang, Meng Liu, Wang Wang, C Michael Crowder
Despite longstanding efforts to develop cytoprotective drugs against ischemia/reperfusion (IR) injuries, there remains no effective therapeutics to treat hypoxic injury. The failure of traditional strategies at solving this problem suggests the need for novel and unbiased approaches that can lead to previously unsuspected targets and lead compounds. Towards this end, we report here a unique small molecule screen in the nematode C. elegans for compounds that improve recovery when applied after the hypoxic insult, using a C...
2017: PloS One
https://www.readbyqxmd.com/read/28426083/energetic-isomers-of-1-2-4-5-tetrazine-bis-1-2-4-triazoles-with-low-toxicity
#6
A Shlomovich, T Pechersky, A Cohen, Q L Yan, M Kosa, N Petrutik, N Tal, A Aizikovich, M Gozin
A series of nitrogen-rich "green" Energetic Materials (EMs), some with improved sensitivity, thermostability, and very low toxicity, were synthesized on the basis of 3,5-diamino-1,2,4-triazole (DAT) and 1,2,4,5-tetrazine building blocks. Since DAT contains several nucleophilic reactive sites, obtaining selective reactivity and specific isomeric products with 1,2,4,5-tetrazine precursors is a challenging task. We developed reaction conditions under which specific isomers could be prepared. On evaluating these compounds for their energetic properties, we found that N(5),N(5)'-(1,2,4,5-tetrazine-3,6-diyl)-bis(1H-1,2,4-triazole-3,5-diamine) 1 has very high thermostability (onset of decomposition temperature at 357 °C) and it is insensitive to impact (Im > 98 J), friction (>360 N) and electrostatic discharge (2512 mJ)...
April 20, 2017: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/28423628/benzyl-isothiocyanate-induces-reactive-oxygen-species-initiated-autophagy-and-apoptosis-in-human-prostate-cancer-cells
#7
Ji-Fan Lin, Te-Fu Tsai, Shan-Che Yang, Yi-Chia Lin, Hung-En Chen, Kuang-Yu Chou, Thomas I-Sheng Hwang
Benzyl isothiocyanate (BITC) in cruciferous plants, which are part of the human diet, has been shown to induce apoptosis in various types of cancer. In this study, we show that BITC effectively suppresses the growth of cultured human prostate cancer cells (CRW-22Rv1 and PC3) by causing mitochondrial membrane potential loss, caspase 3/7 activation and DNA fragmentation. Furthermore, BITC induces ROS generation in these cells. The induction of apoptosis by BITC was significantly attenuated in the presence of N-acetylcysteine (NAC) and catalase (CAT), well-studied ROS scavengers...
March 21, 2017: Oncotarget
https://www.readbyqxmd.com/read/28419749/novel-19-f-mrs-%C3%AE-galactosidase-reporter-molecules-incorporated-nitrogen-mustard-analogues
#8
Zijun Yu, Jianru Zhao, Zhiming Hua, Xinping Wang, Xiaobo Wang, Hanqin Wang, Jian-Xin Yu
In this paper, we propose a novel molecular platform integrated fluorinated antitumor nitrogen mustards for (19) F-MRS assay of β-galactosidase (β-gal) activity. Following this idea, we have designed, synthesized and characterized 2-fluoro-4-[bis(2'-chloroethyl)amino]phenyl β-D-galactopyranoside 5, 2-fluoro-4-{bis[2'-O-(β-D-galactopyranosyl)ethyl]amino}phenyl β-D-galactopyranoside 8, 2-fluoro-4-{bis[[1''-(β-D-galactopyranosyl)-1'', 2'', 3''-triazol-4''-yl]methyl] amino}phenyl β-D-galactopyranoside 14 and 2-fluoro-4-{bis[[1''-(β-D-glucopyranosyl)-1'', 2'', 3''-triazol-4''-yl]methyl]amino}phenyl β-D-galactopyranoside 15 through glycosylation and click reaction strategies, and their structures were confirmed by NMR and HRMS or elemental analysis data...
April 16, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28419580/liquid-liquid-interfacial-synthesis-of-click-nanosheet
#9
Amalia Rapakousiou, Ryo Shiotsuki, Ryota Sakamoto, Ryota Matsuoka, Ukyo Nakajima, Tigmansu Pal, Rintaro Shimada, Md Amran Hossain, Hiroyasu Masunaga, Satoshi Horike, Yasutaka Kitagawa, Sono Sasaki, Kenichi Kato, Takeaki Ozawa, Didier Astruc, Hiroshi Nishihara
A liquid/liquid interfacial synthesis is employed for the first time to synthesize a covalent two-dimensional polymer nanosheet. Copper-catalyzed azide-alkyne cycloaddition (CuAAC) between three-way terminal alkyne and azide at a water/dichloromethane interface generates a 1,2,3-triazole-linked nanosheet. The resultant nanosheet with a flat and smooth texture has a maximum domain size of 20 μm and minimum thickness of 5.3 nm. The starting monomers in the organic phase and the copper catalyst in the aqueous phase can meet together only at the liquid/liquid interface as a two-dimensional reaction space, which allows them to form the two-dimensional polymer...
April 18, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28418188/a-facile-and-versatile-synthesis-of-energetic-furazan-functionalized-5-nitroimino-1-2-4-triazoles
#10
Zhen Xu, Guangbin Cheng, Hongwei Yang, Xuehai Ju, Ping Yin, Jiaheng Zhang, Jean'ne M Shreeve
An analogue-oriented synthetic route for the formulation of furazan-functionalized 5-nitroimino-1,2,4-triazoles has been explored. The process was found to be straightforward, high yielding, and highly efficient, and scalable. Nine compounds were synthesized and the physicochemical and energetic properties, including density, thermal stability, and sensitivity, were investigated, as well as the energetic performance (e.g., detonation velocities and detonation pressures) as evaluated by using EXPLO5 code. Among the new materials, compounds 4-6 and 11 possess high densities, acceptable sensitivities, and good detonation performances, and thereby demonstrate the potential applications as new secondary explosives...
April 18, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28417904/zebrafish-as-an-alternative-vertebrate-model-for-investigating-developmental-toxicity-the-triadimefon-example
#11
Maria Zoupa, Kyriaki Machera
Triadimefon is a widely used triazole fungicide known to cause severe developmental defects in several model organisms and in humans. The present study evaluated in detail the developmental effects seen in zebrafish embryos exposed to triadimefon, confirmed and expanded upon previous phenotypic findings and compared them to those observed in other traditional animal models. In order to do this, we exposed embryos to 2 and 4 µg/mL triadimefon and evaluated growth until 120 h post-fertilization (hpf) through gross morphology examination...
April 12, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28416538/susceptibility-testing-of-common-and-uncommon-aspergillus-species-against-posaconazole-and-other-mold-active-antifungal-azoles-using-the-sensititre-method
#12
Enrica Mello, Brunella Posteraro, Antonietta Vella, Elena De Carolis, Riccardo Torelli, Tiziana D'Inzeo, Paul E Verweij, Maurizio Sanguinetti
We tested 59 common and 27 uncommon Aspergillus species isolates for the susceptibility to the mold-active azole antifungal agents, itraconazole, voriconazole, and posaconazole, using the Sensititre method. The overall essential agreement with the CLSI reference method was 96.5% for itraconazole and posaconazole, and 100% for voriconazole. By Sensititre, as well as CLSI, all of 10 A. fumigatus isolates with a cyp51 mutant genotype were classified as being non-wild-type (MIC > ECV) to triazoles.
April 17, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28414452/cation-exchange-approach-to-tuning-the-flexibility-of-a-metal-organic-framework-for-gated-adsorption
#13
Mingli Deng, Yang Pan, Jiaxing Zhu, Zhenxia Chen, Zhengzong Sun, Jinyu Sun, Yun Ling, Yaming Zhou, Pingyun Feng
Achieving tailorable gated adsorption by tuning the dynamic behavior of a host porous material is of great interest because of its practical application in gas adsorption and separation. Here we devise a unique cation-exchange approach to tune the dynamic behavior of a flexible anionic framework, [Zn2(bptc)(datrz)](-) (denoted as MAC-6, where H4bptc = [1,1'-biphenyl]-3,3',5,5'-tetracarboxylic acid and Hdatrz = 3,5-diamine-1H-1,2,4-triazole), so as to realize the tailorable gated adsorption. The CO2 adsorption amount at 273 K can be enhanced by exchanging the counterion of protonated dimethylamine (HDMA(+)) with tetraethylammonium (TEA(+)), tetrabutylammonium (TBA(+)), and tetramethylammonium (TMA(+)), where the adsorption behavior is transferred from nongated to gated adsorption...
April 17, 2017: Inorganic Chemistry
https://www.readbyqxmd.com/read/28414235/bis-heteroleptic-ruthenium-ii-complex-of-pendant-urea-functionalized-pyridyl-triazole-and-phenathroline-for-recognition-sensing-and-extraction-of-oxyanions
#14
Tamal Kanti Ghosh, Sourav Chakraborty, Bijit Chowdhury, Pradyut Ghosh
A new bis-heteroleptic Ru(II) complex based ditopic receptor, 1[PF6]2, having an anion binding triazole -CH unit and appended 4-fluorophenyl urea arm has been developed. (1)H NMR and isothermal titration calorimetry (ITC) experiments showed binding of 1[PF6]2 toward oxyanions such as phosphates (e.g., H2PO4(-) and HP2O7(3-)) and carboxylates (e.g., CH3CO2(-) and C6H5CO2(-)) anions selectively. (1)H NMR studies showed that highly basic phosphate anions such as HP2O7(3-)/H2PO4(-) are bound by both -CH and -NH units of complex 1[PF6]2...
April 17, 2017: Inorganic Chemistry
https://www.readbyqxmd.com/read/28412813/singlet-oxygen-detection-on-a-nanostructured-porous-silicon-thin-film-via-photonic-luminescence-enhancements
#15
S N Aisyiyah Jenie, Sally E Plush, Nicolas H Voelcker
Because reactive oxygen species are involved in a range of pathologies, developing analytical tools for this group of molecules opens new vistas for biomedical diagnostics. Herein, we fabricate a porous silicon microcavity (pSiMC) functionalized with luminescent singlet oxygen ((1)O2) probe EuA ((Eu(III)-2,2',2″-(10-(2-((4-(2-((4-(2-((anthracen-9-ylmethyl)amino)ethyl)-1H-1,2,3-triazol-1-yl)amino)-2-oxoethyl)-2-oxo-1,2-dihydroquinolin-7-yl)amino)-2-oxoethyl)-1,4,7,10-tetraazacyclododecane-1,4,7-triyl)triacetic acid) as proof of concept of an optical sensor for reactive oxygen species...
April 20, 2017: Langmuir: the ACS Journal of Surfaces and Colloids
https://www.readbyqxmd.com/read/28411406/discovery-of-novel-2-substituted-4-2-fluorophenoxy-pyridine-derivatives-possessing-pyrazolone-and-triazole-moieties-as-dual-c-met-vegfr-2-receptor-tyrosine-kinase-inhibitors
#16
Weijie Gu, Yuxuan Dai, Hao Qiang, Wei Shi, Chen Liao, Fangnuo Zhao, Wenlong Huang, Hai Qian
In our efforts to develop novel dual c-Met/VEGFR-2 inhibitors as potential anticancer agents, a series of 2-substituted-4-(2-fluorophenoxy) pyridine derivatives bearing pyrazolone scaffold were designed and synthesized. The cell proliferation assay in vitro demonstrated that most target compounds had inhibition potency on both c-Met and VEGFR-2, especially compound 9h, 12b and 12d. Based on the further enzyme assay in vitro, compound 12d was considered as the most promising one, the IC50 values of which were 0...
April 8, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28411311/total-fluorescence-fingerprinting-of-pesticides-a-reliable-approach-for-continuous-monitoring-of-soils-and-waters
#17
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/28409630/silver-i-catalyzed-regioselective-synthesis-of-triazole-fused-1-5-benzoxazocinones
#18
Indrajeet J Barve, Tushar Ulhas Thikekar, Chung-Ming Sun
An efficient and regioselective synthesis of novel 1,2,3-triazole-fused-1,5-benzoxazocinones through intramolecular cyclization of substituted ethynyl triazoyl benzoic acids was explored. A crucial precursor 5-iodo-1,2,3-triazole benzoate was obtained from substituted 2-azido benzoic acid esters in a single step through a Copper-Catalyzed Azide-Alkyne Cycloaddition (CuAAC) reaction using a CuI/NBS catalytic system. A carbon-carbon triple bond was installed through a Sonogashira coupling reaction by various terminal alkynes...
April 14, 2017: Organic Letters
https://www.readbyqxmd.com/read/28409338/fluorine-18-labeling-of-the-her2-targeting-single-domain-antibody-2rs15d-using-a-residualizing-label-and-preclinical-evaluation
#19
Zhengyuan Zhou, Ganesan Vaidyanathan, Darryl McDougald, Choong Mo Kang, Irina Balyasnikova, Nick Devoogdt, Angeline N Ta, Brian R McNaughton, Michael R Zalutsky
PURPOSE: Our previous studies with F-18-labeled anti-HER2 single-domain antibodies (sdAbs) utilized 5F7, which binds to the same epitope on HER2 as trastuzumab, complicating its use for positron emission tomography (PET) imaging of patients undergoing trastuzumab therapy. On the other hand, sdAb 2Rs15d binds to a different epitope on HER2 and thus might be a preferable vector for imaging in these patients. The aim of this study was to evaluate the tumor targeting of F-18 -labeled 2Rs15d in HER2-expressing breast carcinoma cells and xenografts...
April 13, 2017: Molecular Imaging and Biology: MIB: the Official Publication of the Academy of Molecular Imaging
https://www.readbyqxmd.com/read/28406541/stereoselective-and-enantiospecific-mono-and-bis-c-h-azidation-of-tr%C3%A3-ger-bases-insight-on-bridgehead-iminium-intermediates-and-application-to-anion-binding-catalysis
#20
Alessandro Bosmani, Sandip Pujari, Laure Guenee, Céline Besnard, Amalia Isabel Poblador Bahamonde, Jerome Lacour
In the context to Tröger base chemistry, regio and stereoselective Csp3-H azidation reactions are reported. Azide functional groups are introduced at either one or the two benzylic positions selectively. Mild conditions and good yields are afforded by the combination of TMSN3 and iodosobenzene PhIO. The process occurs with high enantiospecificity (es 96-99%) and, interestingly and importantly, via bridgehead iminium intermediates as shown by mechanistic and in-silico studies. Finally, mono and bis triazole derivatives were prepared in high yields and enantiospecificity using CuAAC reactions; some of the products being used as anion-binding organocatalysts for the tritylation of amines and alcohols...
April 12, 2017: Chemistry: a European Journal
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