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https://www.readbyqxmd.com/read/28812065/visible-light-induced-cyclization-reactions-for-the-synthesis-of-1-2-4-triazolines-and-1-2-4-triazoles
#1
Hongyu Wang, Yanfei Ren, Kaiye Wang, Yunquan Man, Yanan Xiang, Na Li, Bo Tang
A novel method for concisely synthesizing 1,2,4-triazolines via [3+2] cyclization under visible light is reported. These compounds can be easily converted into 1,2,4-triazoles under basic or photoredox conditions. The application of the 1,2,4-triazoles was also investigated via mild operations.
August 16, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/28811086/proteomic-profiling-of-the-antifungal-drug-response-of-aspergillus-fumigatus-to-voriconazole
#2
Nansalmaa Amarsaikhan, Daniela Albrecht-Eckardt, Christoph Sasse, Gerhard H Braus, Zumrut B Ogel, Olaf Kniemeyer
Antifungal resistance is an emerging problem and one of the reasons for treatment failure of invasive aspergillosis (IA). Voriconazole has become a standard therapeutic for the treatment of this often fatal infection. We studied the differentially expressed proteins as a response of Aspergillus fumigatus to voriconazole by employing the two-dimensional difference gel electrophoresis (DIGE) technique. Due to addition of drug, a total of 135 differentially synthesized proteins were identified by MALDI-TOF/TOF-mass spectrometry...
August 5, 2017: International Journal of Medical Microbiology: IJMM
https://www.readbyqxmd.com/read/28809503/synthesis-of-denser-energetic-metal-organic-frameworks-via-a-tandem-anion-ligand-exchange-strategy
#3
Jichuan Zhang, Hui Su, Yalu Dong, Pengcheng Zhang, Yao Du, Shenghua Li, Michael Gozin, Siping Pang
High-density materials have attracted extensive attention because of their broad applications. However, strategies for improving the densities of MOFs and preparing denser MOFs remain almost unexplored. Herein, we propose a tandem anion-ligand exchange strategy for synthesizing denser MOFs by using three-dimensional cationic MOFs (3D CMOFs) with pillared layered structures as precursors and high-density anions and small monotopic ligands as exogenous guests. By means of this strategy, we choose the high-density nitroformate ion [C(NO2)3(-)] as an exogenous anion and water as an exogenous ligand to successfully synthesize two layered CMOFs...
August 15, 2017: Inorganic Chemistry
https://www.readbyqxmd.com/read/28806568/a-simple-high-performance-liquid-chromatography-mass-spectrometry-method-for-therapeutic-drug-monitoring-of-isavuconazole-and-four-other-antifungal-drugs-in-human-plasma-samples
#4
Giovanna Fatiguso, Fabio Favata, Ilaria Zedda, Amedeo De Nicolò, Jessica Cusato, Valeria Avataneo, Giovanni Di Perri, Antonio D'Avolio
Triazoles chanced the prevention and treatment of invasive fungal infections, but their pharmacokinetic properties are still unclear. In particular, isavuconazole (ISC) is a new broad-spectrum antifungal triazole approved in 2015 as first-line treatment for intravenous and oral use against invasive aspergillosis and for mucormycosis. Nowadays, the optimal management of the treatments with triazoles requires the use of Therapeutic Drug Monitoring (TDM), in order to prevent sub-therapeutic or toxic concentrations...
August 5, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28803043/structure-based-development-of-novel-triazoles-and-related-thiazolotriazoles-as-anticancer-agents-and-cdc25a-b-phosphatase-inhibitors-synthesis-in%C3%A2-vitro-biological-evaluation-molecular-docking-and-in-silico-adme-t-studies
#5
Sherif A F Rostom, Mona H Badr, Heba A Abd El Razik, Hayam M A Ashour
Synthesis of twenty nine new 1,2,4-triazoles and some derived thiazolothiadiazoles (structurally-relevant to some reported triazoles with anticancer and/or Cdc25A/B inhibitory activities) is described in this study. The obtained NCI's in vitro antitumor data revealed that five analogs (12, 15, 18, 19 and 22) displayed considerable tumor percentage growth inhibitory activity (GI%), among which the analog 18 possessed a special antitumor potential and spectrum. Additionally, the same five analogs showed a marginal GI effect on the normal breast epithelial cell line MCF-10A indicating higher selectivity towards cancer cells...
July 25, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28802124/design-synthesis-and-bioevaluation-of-antitubulin-agents-carrying-diaryl-5-5-fused-heterocycle-scaffold
#6
Qile Xu, Maolin Sun, Zhaoshi Bai, Yueting Wang, Yue Wu, Haiqiu Tian, Daiying Zuo, Qi Guan, Kai Bao, Yingliang Wu, Weige Zhang
A series of 3,6-diaryl-1H-pyrazolo[5,1-c][1,2,4]triazoles (I) and 3,6-diaryl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles (II) as antitubulin agents were designed, synthesized and bioevaluated. Compounds (II) 4a, 4d, 4f, 4j, 4l and 4n showed potent antiproliferative activity at sub-micromolar or nanomolar concentrations against SGC-7901, A549 and HT-1080 cell lines, indicating that the bioisosteric replacement of the carbonyl group and B-ring of SMART and ABI with a 5,5-fused-heterocycle scaffold successfully maintained potent antiproliferative activity...
June 1, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28801886/effects-of-3-nitro-1-2-4-triazol-5-one-on-survival-growth-and-metamorphosis-in-the-northern-leopard-frog-lithobates-pipiens
#7
David A Pillard, William S Eck, Mark S Johnson, Stephanie Packard
New explosive formulations are being developed to be less sensitive to impact and inadvertent explosion, increasing safety for the warfighter. Since testing and training make environmental releases imminent, the toxicity of 3-nitro-1,2,4-triazol-5-one (NTO), a component of Insensitive Munitions eXplosive (IMX) formulations, was assessed in a one-generation study to the northern leopard frog (Lithobates ( = Rana) pipiens). Because NTO in water creates acidic conditions, acute studies were conducted with non-pH-adjusted NTO, while a long-term (70-d) study was conducted with neutralized NTO...
August 11, 2017: Ecotoxicology
https://www.readbyqxmd.com/read/28797799/triazole-tethered-isatin-coumarin-based-molecular-hybrids-as-novel-antitubulin-agents-design-synthesis-biological-investigation-and-docking-studies
#8
Harbinder Singh, Jatinder V Singh, Manish K Gupta, Ajit K Saxena, Sahil Sharma, Kunal Nepali, Preet Mohinder S Bedi
In an attempt to develop potent anti-tubulin agents against most dreadful disease cancer, a library of 28 novel triazole tethered isatin-coumarin hybrids were synthesized by click chemistry approach. Synthesized hybrids were characterized and evaluated against a panel of human cancer cell lines viz. THP-1, COLO-205, HCT-116 and PC-3. Biological assay unveiled that, compounds A-1 to A-6, B-1 to B-4 and C-1 to C-3 displayed significant inhibitory potential against THP-1, COLO-205 and HCT-116 cell lines which were more sensitive towards the designed hybrids...
July 29, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28797773/methyl-propiolate-and-3-butynone-starting-points-for-synthesis-of-amphiphilic-1-2-3-triazole-peptidomimetics-for-antimicrobial-evaluation
#9
Thomas A Bakka, Morten B Strøm, Jeanette H Andersen, Odd R Gautun
A library of 29 small 1,4-substituted 1,2,3-triazoles was prepared for studies of antimicrobial activity. The pharmacophore model investigated with these substrates was based on small peptidomimetics of antimicrobial peptides and antimicrobials isolated from marine organisms from sub-arctic regions. Using methyl 1,2,3-triazole-carboxylates and 1,2,3-triazole methyl ketones prepared through "click" chemistry we were able to synthesize the different cationic amphiphiles through three steps or less. Several structural modifications to the lipopohilic side and hydrophilic sides of the amphiphiles were investigated and compared with regards to antimicrobial activity and cytotoxicity in particular...
July 29, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28796504/ligand-configuration-induced-manganese-ii-coordination-polymers-syntheses-crystal-structures-sorption-and-magnetic-properties
#10
Wen-Juan Shi, Li-Yun Du, Hong-Yun Yang, Kun Zhang, Lei Hou, Yao-Yu Wang
Three new coordination polymers, {[Mn3(pzbtz)2(Cl)2(H2O)2]·4H2O}n (1), {Mn2(pzbtz)(SO4)(H2O)3]·3H2O}n (2), and {[Mn3(pzbtz)3(H2O)3]·1.5DMA·2H2O}n (3), have been solvothermally synthesized with MnCl2/MnSO4 and a bitriazole ligand, 5'-(pyrazin-2-yl)-2H,4'H-3,3'-bi(1,2,4-triazole) (H2pzbtz), in different solvent systems. H2pzbtz shows different geometrical configurations and coordination modes, leading to the diverse three-dimensional (3D) frameworks of 1-3. Complex 1 contains the trinuclear Mn3(tr)4X2 (X = Cl or H2O) clusters and reveals an unobserved (3,4,8)-connected sqc929 topological framework with two types of cages...
August 10, 2017: Inorganic Chemistry
https://www.readbyqxmd.com/read/28795298/pharmacokinetics-of-azole-antifungals-in-cystic-fibrosis
#11
REVIEW
Ryan M Rivosecchi, Palash Samanta, Moses Demehin, M Hong Nguyen
Defects in mucociliary clearance predispose cystic fibrosis (CF) patients to airway colonization and infection by various fungi, especially Aspergillus fumigatus. Although the clinical significance of airway fungal colonization is not clear, several studies have suggested its association with worsening lung function and increased risk of CF exacerbations. Antifungal triazole agents have been used in CF patients with airway fungal colonization or infections with varying results. Limited pharmacokinetic studies to date have demonstrated high inter-subject variability of triazole levels among CF patients...
August 9, 2017: Mycopathologia
https://www.readbyqxmd.com/read/28791908/synthesis-and-biological-evaluation-of-novel-7-hydroxy-4-phenylchromen-2-one-linked-to-triazole-moieties-as-potent-cytotoxic-agents
#12
Chuan-Feng Liu, Qing-Kun Shen, Jia-Jun Li, Yu-Shun Tian, Zheshan Quan
A new series of novel 7-hydroxy-4-phenylchromen-2-one (1a)-linked 1,2,4-triazoles were synthesised using a click chemistry approach. All derivatives were subjected to 3-(4,5-dimethylthiazol-yl)-diphenyl tetrazolium bromide (MTT) cytotoxicity screening against a panel of six different human cancer cell lines (AGS, MGC-803, HCT-116, A-549, HepG2, and HeLa) to assess their cytotoxic potential. Among the tested molecules, some of the analogues showed better cytotoxic activity than that shown by the 7-hydroxy-4-phenylchromen-2-one (1a)...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28783127/tuning-sensory-properties-of-triazole-conjugated-spiropyrans-metal-ion-selectivity-and-paper-based-colorimetric-detection-of-cyanide
#13
Juhyen Lee, Eun Jung Choi, Inwon Kim, Minhe Lee, Chinnadurai Satheeshkumar, Changsik Song
Tuning the sensing properties of spiropyrans (SPs), which are one of the photochromic molecules useful for colorimetric sensing, is important for efficient analysis, but their synthetic modification is not always simple. Herein, we introduce an alkyne-functionalized SP, the modification of which would be easily achieved via Cu-catalyzed azide-alkyne cycloaddition ("click reaction"). The alkyne-SP was conjugated with a bis(triethylene glycol)-benzyl group (EG-BtSP) or a simple benzyl group (BtSP), forming a triazole linkage from the click reaction...
August 7, 2017: Sensors
https://www.readbyqxmd.com/read/28780468/design-and-synthesis-of-2-6-di-substituted-phenyl-thiazolo-3-2-b-1-2-4-triazoles-as-%C3%AE-glucosidase-and-%C3%AE-amylase-inhibitors-co-relative-pharmacokinetics-and-3d-qsar-and-risk-analysis
#14
Pervaiz Ali Channar, Aamer Saeed, Fayaz Ali Larik, Sajid Rashid, Qaiser Iqbal, Maryam Rozi, Saima Younis, Jamaluddin Mahar
Ten fused heterocyclic derivatives bearing the 2,6-di(subsituted phenyl)thiazolo[3,2-b]-1,2,4-triazoles as central rings were synthesized and structures of the compounds were established by analytical and spectral data using FTIR, EI-MS, (1)H NMR and (13)C NMR techniques. In vitro inhibitory activities of synthesized compounds on α-amylase, α-glucosidase and α-burylcholinesterase (α-BuChE) were evaluated using a purified enzyme assays. Compound 5c demonstrated strong and selective α-amylase inhibitory activity (IC50=1...
August 3, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28777537/pushing-chemical-boundaries-with-n-heterocyclic-olefins-nhos-from-catalysis-to-main-group-element-chemistry
#15
Matthew M D Roy, Eric Rivard
N-Heterocyclic olefins (NHOs) have gone from the topic of a few scattered (but important) reports in the early 1990s to very recently being a ligand/reagent of choice in the far-reaching research fields of organocatalysis, olefin and heterocycle polymerization, and low oxidation state main group element chemistry. NHOs are formally derived by appending an alkylidene (CR2) unit onto an N-heterocyclic carbene (NHC), and their pronounced ylidic character leads to high nucleophilicity and soft Lewis basic character at the ligating carbon atom...
August 4, 2017: Accounts of Chemical Research
https://www.readbyqxmd.com/read/28776447/analysis-of-imidazoles-and-triazoles-in-biological-samples-after-microextraction-by-packed-sorbent
#16
Cristina Campestre, Marcello Locatelli, Paolo Guglielmi, Elisa De Luca, Giuseppe Bellagamba, Sergio Menta, Gokhan Zengin, Christian Celia, Luisa Di Marzio, Simone Carradori
This paper reports the MEPS-HPLC-DAD method for the simultaneous determination of 12 azole drugs (bifonazole, butoconazole, clotrimazole, econazole, itraconazole, ketoconazole, miconazole, posaconazole, ravuconazole, terconazole, tioconazole and voriconazole) administered to treat different systemic and topical fungal infections, in biological samples. Azole drugs separation was performed in 36 min. The analytical method was validated in the ranges as follows: 0.02-5 μg mL(-1) for ravuconazole; 0.2-5 μg mL(-1) for terconazole; 0...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28774702/candida-and-invasive-mould-diseases-in-non-neutropenic-critically-ill-patients-and-patients-with-haematological-cancer
#17
REVIEW
A L Colombo, J N de Almeida Júnior, Monica A Slavin, Sharon C-A Chen, Tania C Sorrell
Critically ill patients and patients with haematological cancer are HIV-negative populations at high risk of invasive fungal infections. In intensive-care units, candidaemia and intra-abdominal candidiasis predominate, but aspergillosis has emerged as a lethal, under-recognised cause of pneumonia. In patients with haematological malignancies or who have undergone stem-cell transplantations, pulmonary disease due to aspergillus and other mould diseases predominate. In this Series paper, we provide an update on risk assessment, new diagnostic strategies, and therapeutic approaches...
July 31, 2017: Lancet Infectious Diseases
https://www.readbyqxmd.com/read/28773931/charged-triazole-cross-linkers-for-hyaluronan-based-hybrid-hydrogels
#18
Maike Martini, Patricia S Hegger, Nicole Schädel, Burcu B Minsky, Manuel Kirchhof, Sebastian Scholl, Alexander Southan, Günter E M Tovar, Heike Boehm, Sabine Laschat
Polyelectrolyte hydrogels play an important role in tissue engineering and can be produced from natural polymers, such as the glycosaminoglycan hyaluronan. In order to control charge density and mechanical properties of hyaluronan-based hydrogels, we developed cross-linkers with a neutral or positively charged triazole core with different lengths of spacer arms and two terminal maleimide groups. These cross-linkers react with thiolated hyaluronan in a fast, stoichiometric thio-Michael addition. Introducing a positive charge on the core of the cross-linker enabled us to compare hydrogels with the same interconnectivity, but a different charge density...
September 30, 2016: Materials
https://www.readbyqxmd.com/read/28773020/warm-white-light-emitting-diodes-based-on-a-novel-orange-cationic-iridium-iii-complex
#19
Huaijun Tang, Guoyun Meng, Zeyu Chen, Kaimin Wang, Qiang Zhou, Zhengliang Wang
A novel orange cationic iridium(III) complex [(TPTA)₂Ir(dPPOA)]PF₆ (TPTA: 3,4,5-triphenyl-4H-1,2,4-triazole, dPPOA: N,N-diphenyl-4-(5-(pyridin-2-yl)-1,3,4-oxadiazol-2-yl)aniline) was synthesized and used as a phosphor in light-emitting diodes (LEDs). [(TPTA)₂Ir(dPPOA)]PF₆ has high thermal stability with a decomposition temperature (Td) of 375 °C, and its relative emission intensity at 100 °C is 88.8% of that at 25°C. When only [(TPTA)₂Ir(dPPOA)]PF₆ was used as a phosphor at 6.0 wt % in silicone and excited by a blue GaN (GaN: gallium nitride) chip (450 nm), an orange LED was obtained...
June 16, 2017: Materials
https://www.readbyqxmd.com/read/28772698/a-series-of-robust-copper-based-triazolyl-isophthalate-mofs-impact-of-linker-functionalization-on-gas-sorption-and-catalytic-activity-%C3%A2
#20
Ulrike Junghans, Merten Kobalz, Oliver Erhart, Hannes Preißler, Jörg Lincke, Jens Möllmer, Harald Krautscheid, Roger Gläser
The synthesis and characterization of an isomorphous series of copper-containing microporous metal-organic frameworks (MOFs) based on triazolyl isophthalate linkers with the general formula [Cu₄(μ₃-OH)₂(R¹-R²-trz-ia)₃(H₂O)x] are presented. Through size adjustment of the alkyl substituents R¹ and/or R² at the linker, the impact of linker functionalization on structure-property relationships was studied. Due to the arrangement of the substituents towards the cavities, the porosity (pore fraction 28%-39%), as well as the pore size can be adjusted by the size of the substituents of the triazole ring...
March 24, 2017: Materials
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