TY - JOUR. T1 - Evaluation of positive inotropic activity induced by a triazole derivative using an isolated heart model. AU - Lauro, Figueroa Valverde. AU - Francisco, Díaz Cedillo. AU - Elodia, García Cervera. AU - Eduardo, Pool Gómez. AU - Maria, López Ramos. AU - Marcela, Rosas Nexticapa. AU - Lenin, Hau Heredia. AU - Betty, Sarabia Alcocer. AU - Velázquez-Sarabia, Betty M.. PY - 2014/1/1. Y1 - 2014/1/1. N2 - There are some reports which indicate that several triazole derivatives have inotropic activity; however, the cellular site and mechanism of action at cardiovascular level is very confusing. In order, to have a clear understanding of these phenomena, a triazole derivative was synthesized to evaluate its biological activity on left ventricular pressure and characterize the molecular mechanism. The Langendorff technique was used to measure changes on perfusion pressure and coronary resistance in an isolated rat heart model in absence or presence of the triazole derivative. ...
TY - JOUR. T1 - In vitro susceptibilities of yeasts to a new antifungal triazole, SCH 39304. T2 - Effects of test conditions and relation to in vivo efficacy. AU - McIntyre, K. A.. AU - Galgiani, J. N.. PY - 1989/1/1. Y1 - 1989/1/1. N2 - We used six candidal strains (two Candida albicans and one each of four other species) to study the effects of test conditions on the activity of SCH 39304 compared with that of fluconazole in broth macro- and microdilution assays. Increasing the inoculum from 102 to 105 yeasts per ml raised the MICs for all isolates up to , 512-fold. In contrast, results with a 50% turbidimetric endpoint (50% inhibitory concentration; IC( 1/2 )) varied no more than twofold. Similar effects were seen with fluconazole, and both drugs were found to have an associated delay in onset of action. Acidity was found to increase both MICs and IC( 1/2 )s. Other effects were observed among four synthetic media, but a consistent pattern was not identified. Incubation temperatures of 37, 35 ...
OBJECTIVES:. I. Determine the toxicity and disease-stabilizing effect of carboxyamidotriazole in patients with metastatic renal cell carcinoma.. II. Determine the objective response rate in patients treated with this drug.. OUTLINE: This is a randomized, double-blind, multicenter study. Patients are stratified according to time from diagnosis of metastatic disease to study entry (fewer than 24 months vs 24 months or more).. Patients receive oral carboxyamidotriazole (CAI) daily for 4 weeks. Treatment repeats for 4 courses in the absence of disease progression or unacceptable toxicity. After 4 courses, patients experiencing complete or partial response continue treatment until disease progression or unacceptable toxicity.. Patients with stable disease are randomized to one of two treatment arms.. Arm I: Patients receive oral CAI as above.. Arm II: Patients receive a placebo.. Treatment repeats every 4 weeks for at least 4 courses in the absence of disease progression or unacceptable toxicity. ...
This post introduces the properties and mechanism of benzotriazole corrosion inhibitors(anchor). The synergistic action of benzotriazole and imidazole better illustrates the progress of sustained release.
A wide range of stable vinyl selenone-modified furanosides has been synthesized for the first time. These 2π-partners undergo 1,3-dipolar cycloaddition reactions with a wide range of organic azides to afford enantiopure trisubstituted triazoles. Furanosyl rings opened up during triazole synthesis to generate polyfunctionalized molecules, ready to undergo further transformations. This strategy is one of the most convenient methods for the synthesis of enantiopure 1,4,5-trisubstituted 1,2,3-triazoles where the chiral components are attached to C-4 or C-5 position of triazole ring. These triazoles are formed in a regioselective manner, and several pairs of regioisomeric triazoles have also been synthesized. The approach affords densely functionalized triazoles, which are amenable to further modifications because of the presence of aldehyde and hydroxyl groups. This powerful and practical route adds to the arsenals of chemists and biologists interested in the synthesis and applications of triazoles. ...
Liquid electrolyte consisting of 1 M LiPF6 in ethylene carbonate (EC)/dimethyl carbonate (DMC) and 0.1 wt% benzotriazole (BzTz) is studied in |TEX|$LiCoO_2$|/TEX|//graphite battery system at room temperature. Benzotriazole addition introduces excellent electrochemical stability (5.6 V vs Li) and good ionic conductivity properties at room temperature. Also, this electrolyte shows good cycling performance and better discharge capacities at high C-rates relative to the pristine electrolyte. Furthermore, the additive allows the formation of a good solid electrolyte interphase (SEI) per cyclic voltammetry (CV) examination. These specialized properties make this liquid electrolyte ideal for high power and high voltage applications.
Abstract : Triazoles are an important class of compounds used as core molecule for the synthesis of many pharmaceutical drugs. The objective of the present research was to investigate the influence of biofield treatment on physical, spectral and thermal properties of 1,2,4-triazole. The study was performed in two groups, control and treatment. The control group remained as untreated, and biofield treatment was given to treatment group. The control and treated 1,2,4-triazole were characterized by X-ray diffraction (XRD), Differential Scanning Calorimetry (DSC), Thermo Gravimetric analysis (TGA), Surface area analyzer, and Fourier transform infrared (FT-IR) spectroscopy. XRD analysis revealed a decrease in unit cell volume of treated 1,2,4-triazole (662.08 10-24 cm3) as compared to control sample (666.34 10-24 cm3). Similarly, a decrease in molecular weight of treated 1,2,4-triazole (69.78 g/mol) with respect to control (70.23 g/mol) was observed. Additionally, a substantial decrease in ...
TY - JOUR. T1 - Variable magnitude of drug interaction between oral voriconazole and cyclosporine A in recipients of allogeneic hematopoietic stem cell transplantation. AU - Kikuchi, Taku. AU - Mori, Takehiko. AU - Yamane, Akiko. AU - Kato, Jun. AU - Kohashi, Sumiko. AU - Okamoto, Shinichiro. PY - 2012/9/1. Y1 - 2012/9/1. N2 - Drug interaction between voriconazole and calcineurin inhibitors is often problematic after allogeneic hematopoietic stem cell transplantation (HSCT) or solid organ transplantation. We previously demonstrated an unpredictable inter-individual variability in the magnitude of this drug interaction; however, the route of drug administration was not taken into account. In this study, the drug interaction between voriconazole and calcineurin inhibitors was further analyzed under the condition that both agents were administered orally. Twenty adult recipients of HSCT who had already been on a steady dose of oral cyclosporine A (CsA) and were started on oral voriconazole (400 ...
This population-pharmacokinetics analysis involving adult patients with invasive fungal infections challenges recommended voriconazole dosing regimens. Higher oral than intravenous doses, followed by individualized adjustments based on therapeutic drug monitoring, are needed to improve achievement of the therapeutic target for maximizing response by minimizing neurotoxicity.Background. Recommended oral voriconazole (VRC) doses are lower than intravenous doses. Because plasma concentrations impact efficacy and safety of therapy, optimizing individual drug exposure may improve these outcomes.Methods. A population pharmacokinetic analysis (NONMEM) was performed on 505 plasma concentration measurements involving 55 patients with invasive mycoses who received recommended VRC doses.Results. A 1-compartment model with first-order absorption and elimination best fitted the data. VRC clearance was 5.2 L/h, the volume of distribution was 92 L, the absorption rate constant was 1.1 hourâˆ1, and oral ...
JF-90G:Bis(2,2,6,6-tetramethyl-4-piperidyl)sebacate:Product List:Benzotriazole Compounds«Since the company was founded in 1957, Johoku Chemical has been providing phosphorous compounds, which are used in a variety of fields and applications, such as improving the heat resistance of plastics, fiber and rubber; serving as an antioxidant and modifier; and enhancing the extreme pressure profile of lubricant oil. In addition, Johoku products are now being used in intermediates for medical, agricultural and pharmaceutical industry applications.
Article Photocatalysis assisted by peroxymonosulfate and persulfate for benzotriazole degradation: effect of pH on sulfate and hydroxyl radicals. Recently, notable attempts have been devoted to removing emerging pollutants from water resources. Benzo...
J Pediatric Infect Dis Soc. 2020 Nov 2:piaa119. doi: 10.1093/jpids/piaa119. Online ahead of print.. ABSTRACT. BACKGROUND: Children and adolescents undergoing allogeneic hematopoietic cell transplantation (HCT) are at high risk for invasive fungal disease (IFD).. METHODS: This multicenter, randomized, open-label trial planned to enroll 560 children and adolescents (3 months to ,21 years) undergoing allogeneic HCT between April 2013 and September 2016. Eligible patients were randomly assigned to antifungal prophylaxis with caspofungin or a center-specific comparator triazole (fluconazole or voriconazole). Prophylaxis was administered from day 0 of HCT to day 42 or discharge. The primary outcome was proven or probable IFD at day 42 as adjudicated by blinded central review. Exploratory analysis stratified this evaluation by comparator triazole.. RESULTS: A planned futility analysis demonstrated a low rate of IFD in the comparator triazole arm, so the trial was closed early. A total of 290 eligible ...
If 1,2,3-Triazoles are well known for their biological properties, particular attention has been recently devoted to the development of 2-pyridyl-1,2,3-triazole derivatives (or pyta) as alternative ligands to 2,2-bipyridines. This interest is explained by the easy preparation of such ligands using a click chemistry strategy (Obata et al., 2008; Schweinfurth et al., 2008), and the use of pyta derivatives as efficient chelator systems for Tc(CO)3+ or Re(CO)3+ organometallic cores (Boulay et al., 2010; Seridi et al., 2011). Recently, structural pyta isomers like 4-pyridyl-1,2,3-triazole have been described as building blocks in the synthesis of chelating agents for biomedical applications (Bonnet et al., 2012; Pellegatti et al., 2008). In this paper, we report on the first X-ray structure analysis of a 4-pyridyl-1,2,3-triazole derivative.. The title molecule, Fig. 1, can be considered as a ditopic ligand with two distinct transition metal complexing sites, the iminodiacetate (IDA) pincer and the ...
A series of novel purine-based fluoroaryl triazoles were synthesized using the Cu(I) catalyzed 1,3-dipolar cycloaddition reactions (click reactions), and assayed for their neuroprotective effects using fluorescence electron microscopy. Among these triazoles, o-fluorophenylmetyl-triazole, 7, has comparable neuroprotective effect as that of Flavopiridol (1) and Roscovitine (2), the state of the art CDK inhibitors, against the Aß induced neurotoxicity. These results are substantiated using computer docking methods (DarwinDock/GenDock), which predict that Roscovitine and the triazole 7 bind to the ATP-binding site of CDK5/p25 with comparable binding energies, whereas the corresponding pentafluorophenylmethyl-triazole, 9, has dramatically reduced binding energy (in accordance with its lack of neuroprotection). These combined experimental and theoretical studies support the involvement of CDK5/p25 in the neuronal cell cycle re-entry.
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Page contains details about Nα-biotinyl-Nβ-dansyl-N-(11-azido-3,6,9-trioxaundecyl)-lysine amide triazole-linked to phenyl sulfonamide coated iron nanoparticles . It has composition images, properties, Characterization methods, synthesis, applications and reference articles : nano.nature.com
Aryl azides were treated with allenylmagnesium bromide to generate 1,5-disubstituted butynyl 1,2,3-triazoles in a domino fashion, which upon Cu(I) catalyzed 1,3-dipolar cycloaddition with aryl azides afforded novel bis-1,2,3-triazoles in quantitative yields. The final products were analyzed for their antimicrobial activities against a panel of bacterial and fungal strains which revealed the products to be potent antimicrobials.
The present work deals with the pharmacological screening of some newly synthesized triazoles. A series of 1,2,4-triazoles have been synthesized using benzoic acid or 4-chloro benzoic acid as the...
Download and Read online Advances In Triazole Chemistry, ebooks in PDF, epub, Tuebl Mobi, Kindle Book. Get FreeAdvances In Triazole Chemistry Textbook and unlim
Triazolyl RuII, RhIII, OsII, and IrIII Complexes as Potential Anticancer Agents: Synthesis, Structure Elucidation, Cytotoxicity, and DNA Model Interaction Studies. Organometallics, 2019
This patent search tool allows you not only to search the PCT database of about 2 million International Applications but also the worldwide patent collections. This search facility features: flexible search syntax; automatic word stemming and relevance ranking; as well as graphical results.
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Subjects will be admitted to the clinical research unit on Day 0. Subjects will receive anidulafungin intravenously in a loading dose of 200 mg on Day 1, followed by maintenance doses of 100 mg Q24h on Day 2 and Day 3. Simultaneously, using a separate intravenous access, subjects will receive voriconazole in a loading dose of 6 mg/kg Q12h on Day 1, followed by a maintenance dose of 4 mg/kg Q12h on Day 2, and a 4 mg/kg morning dose on Day 3 ...
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Continuous-flow processing offers unprecedented opportunities to accelerate, integrate, simplify, scale-up and automatize chemical reactions, in combination with an inherently safer and greener nature over traditional batch-based syntheses. Triazoles are amongst the most important and most intensively stud
1H-1,2,4-Triazole, 1,3,5-triphenyl- | C20H15N3 | CID 563249 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
Some 3-thioxo/alkylthio-1,2,4-triazoles with a substituted thiourea moiety as possible antimycobacterials.: A series of novel N-alkyl/aryl-N-[4-(4-alkyl/aryl-2
A library of 1-(1,2,3,3,4,4,6-hepta-O-acetyl-6-deoxy-sucros-6-yl)-1,2,3-triazoles have been investigated for their antibacterial, antifungal and cytotoxic activities. Most of the target compounds showed good inhibitory activity against a variety of clinically and food contaminant important microbial pathogens. In particular, 1-(1,2,3,3,4,4,6-hepta-O-acetyl-6-deoxy-sucros-6-yl)-4-(4-pentylphenyl)-1,2,3-triazole (5) was highly active against all the tested bacteria with minimal inhibitory concentrations (MICs) ranging between 1.1 and 4.4 µM and bactericidal concentrations (MBCs) from 2.2 and 8.4 µM. The compound 1-(1,2,3,3,4,4,6-hepta-O-acetyl-6-deoxy-sucros-6-yl)-4-(4-bromophenyl)-1,2,3-triazole (3) showed antifungal activity with MICs from 0.6 to 4.8 µM and minimal fungicidal concentrations (MFCs) ranging between 1.2 and 8.9 µM. Furthermore, some of the compounds possessed moderate cytotoxicity against human breast, lung, cervical and hepatocellular carcinoma cell lines, ...
1724 Cyclooxygenase-2 (COX-2) inhibitors and calcium influx inhibitors are agents which have previously shown to have cytostatic effects against tumor cells. There is evidence that cyclooxygenase-2 (COX-2) and calcium are both important components of the same pathways that drive the malignant phenotype, including epithelial cell proliferation and inhibition of apoptosis. This intrinsic link between COX-2 and calcium-regulated signaling led to the hypothesis that a COX-2 inhibitor and a calcium influx inhibitor could act cooperatively as anticancer agents. Cytostatic doses of LM-1685, a COX-2 inhibitor, and carboxyamido-triazole (CAI), a voltage-independent calcium channel (VICC) inhibitor, reduced the proliferation and survival of seven different human cancer cell lines by at least one log (p = 0.01) over either agent alone. Time course experiments show that the LM-1685/CAI combination initially suppresses the ERK pathway but ultimately results in high, sustained activation of ERK (p = 0.0005). ...
A triazole antifungal drug that is used to treat invasive infections by Candida species and Aspergillus species in severely immunocompromised patients.
by Papadopoulou MV, Bloomer WD, Rosenzweig HS, Chatelain E, Kaiser M, Wilkinson SR, McKenzie C, and Ioset JR. Journal of Medicinal Chemistry, May 2012
About itraconazolea synthetic triazole derivative, systemic antifungal.mechanism of action of itraconazoleitraconazole is a fungicidal or fungistatic
Analogues structuraux des porphyrines et des Salens, des ligands de type dipyrrométhène bis-phénol ont été étudiés dans notre groupe, notamment sous forme de complexes pour la catalyse doxydation. Lactivité catalytique de ces complexes étant faible, il a été proposé de remplacer les phénols par des triazoles. Lobjet de cette thèse était détudier et de valoriser une nouvelle famille de ligands dipyrrométhène bis-triazole.Plusieurs voies de synthèse ont dabord été étudiées et optimisées pour accéder à ces nouveaux ligands. Nous nous sommes attachés ensuite à valoriser ces nouveaux ligands selon plusieurs axes.Un de ces ligands a été testé en reconnaissance danions, ainsi que les dérivés monotriazolium et bis-triazolium. Les triazoliums ont également permis laccès à des métallocomplexes carbéniques, qui ont été étudiés.Par ailleurs, les métallocomplexes des dipyrrométhène bis-triazole ont été préparés et caractérisés, y compris par ...
A modification of formula D-163 for high temperature processing at temperatures up to 32C. Add 25ml of 0.1% volume/weight solution of benzotriazole in ethylene glycol to each litre of working strength D-163 solution. At temperatures above 24C, print exposure should be adjusted to give a development time of about 1 minute. ...
and thus contain both enantiomers of 2 (see Fig. S2‡). The pseudopeptide rings in 2(rac)2·DHPP2 adopt similar conformations, again with a lower than the ideal C4 symmetry, independent of whether the DHPP dimer is complexed by the all-R or the all-S-enantiomer of 2. The binding modes detected in the structure in Fig. 1 are retained in 2(rac)2·DHPP2. Specifically, the vacant oxygen atoms of the DHPP dimer hydrogen-bond to NH groups of 2 with N⋯O distances ranging between 2.74 and 2.84 Å for all-R-2 and 2.71 and 2.86 Å for all-S-2. Moreover, pairs of opposing triazole CH bonds in the pseudopeptide sandwiches are oriented towards the oxygen atoms of the anion dimer that are involved in the hydrogen-bonding interactions (C⋯O distances for all-R-2: 3.62-4.09 Å and all-S-2: 3.61-4.36 Å), while the other four triazole CH bonds face the bridging oxygen atom of the anions (C⋯O distances for all-R-2: 3.65-3.72 Å and all-S-2: 3.71-3.80 Å). The O⋯O distances in the DHPP dimers amount to ...
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Data collection: SMART Bruker, 2007; cell refinement: SAINT Bruker, 2007; data reduction: SAINT; programs used to solve structure: SHELXS97 Sheldrick, 2008; programs used to refine
An electrical device in provided having two electrodes separated from one another, wherein one temperature controlled electronic spin-state transition particle is in direct contact with each of the t
The synthesis and anticancer properties of 2-(4-amino-5-methyl-4H-[1,2,4]triazol-3-ylsulfanyl)-N-(5-R-benzylthiazol-2-yl)-acetamides
Learn more about 1-Phenyl-1H-1,2,4-triazol-3-ol. We enable science by offering product choice, services, process excellence and our people make it happen.
3,5-Dimethyl-4H-1,2,4-triazol-4-amine | C4H8N4 | CID 229800 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
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TY - JOUR. T1 - Updated results from MONALEESA-2, a phase III trial of first-line ribociclib plus letrozole versus placebo plus letrozole in hormone receptor-positive, HER2-negative advanced breast cancer. AU - Hortobagyi, Gabriel N.. AU - Stemmer, S. M.. AU - Burris, H. A.. AU - Yap, Y. S.. AU - Sonke, G. S.. AU - Paluch-Shimon, S.. AU - Campone, M.. AU - Petrakova, K.. AU - Blackwell, K. L.. AU - Winer, E. P.. AU - Janni, W.. AU - Verma, S.. AU - Conte, P.. AU - Arteaga, C. L.. AU - Cameron, D. A.. AU - Mondal, S.. AU - Su, F.. AU - Miller, M.. AU - Elmeliegy, M.. AU - Germa, C.. AU - OShaughnessy, J.. PY - 2018/7/1. Y1 - 2018/7/1. N2 - Background: The phase III MONALEESA-2 study demonstrated significantly prolonged progression-free survival (PFS) and a manageable toxicity profile for first-line ribociclib plus letrozole versus placebo plus letrozole in patients with hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) advanced breast cancer. Here, we ...
Title:Synthesis and Antifungal Activity Evaluation of New 1,2,4-Triazole Derivatives Bearing Salicylidene Hydrazide Moiety. VOLUME: 13 ISSUE: 2. Author(s):Seref Demirayak, Ismail Kayagil, Leyla Yurttas and Sevda Er. Affiliation:Department of Pharmaceutical Chemistry School of Pharmacy Medipol University 34810 Istanbul Turkey.. Keywords:Salicylidene hydrazide, 1, 2, 4-triazole, antifungal activity.. Abstract:A series of new N-(arylidene)-2-[(1-(4-nitrophenyl)-1H-1,2,4-triazol-3-yl)oxy]acetohydrazide derivatives (1- 16) were prepared and tested for theira ntifungal activity against six plant pathogens, three human pathogens and two nonpathogen microorganisms. The target compounds were obtained with a multi-step reaction starting from 4- substitutedarylhydrazine derivatives and the structures of final compounds have been elucidated with IR, NMR, Mass spectroscopy data and elemental analysis results. The antifungal activity of the compounds was determined against eleven different Fusarium, ...
Purpose The Letrozole (Femara) Versus Anastrozole Clinical Evaluation (FACE) study compared the efficacy and safety of adjuvant letrozole versus anastrozole in postmenopausal patients with hormone receptor (HR) -positive and node-positive early breast cancer (eBC). Methods Postmenopausal women with HR-positive and node-positive eBC were randomly assigned to receive adjuvant therapy with either letrozole (2.5 mg) or anastrozole (1 mg) once per day for 5 years or until recurrence of disease. Patients were stratified on the basis of the number of lymph nodes and human epidermal growth factor receptor 2 status. The primary end point was 5-year disease-free survival (DFS), and the key secondary end points were overall survival and safety. Results A total of 4,136 patients were randomly assigned to receive either letrozole (n = 2,061) or anastrozole (n = 2,075). The final analysis was done at 709 DFS events (letrozole, 341 [16.5%]; anastrozole, 368 [17.7%]). The 5-year estimated DFS rate was 84.9% for ...
TY - JOUR. T1 - Voriconazole, an antifungal triazol that causes visual side effects, is an inhibitor of TRPM1 and TRPM3 channels. AU - Xiong, Wei Hong. AU - Lane Brown, R.. AU - Reed, Brian. AU - Burke, Neal S.. AU - Duvoisin, Robert M.. AU - Morgans, Catherine W.. N1 - Publisher Copyright: © 2015 The Association for Research in Vision and Ophthalmology, Inc.. PY - 2015/2. Y1 - 2015/2. N2 - PURPOSE. Administration of voriconazole, an antifungal triazole, causes transient visual disturbances in patients and attenuates the b-wave of the ERG. We sought to identify the retinal target of voriconazole underlying the effect on the ERG b-wave. METHODS. Electroretinograms were recorded from mice before and after intraperitoneal injection of voriconazole. The effect of voriconazole on ON-bipolar cells was tested by patchclamp recordings of ON-bipolar cells in mouse retinal slices. Effects of voriconazole on mGluR6 and TRPM3 were assessed by patch-clamp recordings of Chinese hamster ovary (CHO) and HEK293 ...
16. A compound according to claim 1, which is: 3-(2-chloro-6-fluorobenzylthio)-5-phenylthiazolo[2,3-c][1,2,4]triazole; 3-(benzo[d][1,3]dioxol-5-ylmethylthio)-5-phenylthiazolo[2,3-c][1,2,4]tria- zole; 3-(3,5-dimethoxybenzylthio)-5-phenylthiazolo[2,3-c][1,2,4]triazole; 3-(4-fluorobenzylthio)-5-phenylthiazolo[2,3-c][1,2,4]triazole; 5-phenyl-3-(4-(trifluoromethyl)benzylthio)thiazolo[2,3-c][1,2,4]triazole; 3-(benzo[d][1,3]dioxol-5-ylmethylthio)-5-(4-chlorophenyl)thiazolo[2,3-c][- 1,2,4]triazole; 3-(benzo[d][1,3]dioxol-5-ylmethylthio)-5-(4-fluorophenyl)thiazolo[2,3-c][- 1,2,4]triazole; 3-((5-phenylthiazolo[2,3-c][1,2,4]triazol-3-ylthio)methyl)phenol; 3-(4-chlorobenzylthio)-5-phenylthiazolo[2,3-c][1,2,4]triazole; 3-(3-chloro-4-methoxybenzylthio)-5-phenylthiazolo[2,3-c][1,2,4]triazole; 3-(2,4-difluorobenzylthio)-5-phenylthiazolo[2,3-c][1,2,4]triazole; 5-phenyl-3-(2-(trifluoromethyl)benzylthio)thiazolo[2,3-c][1,2,4]triazole; 3-(phenethylthio)-5-phenylthiazolo[2,3-c][1,2,4]triazole; ...
The drug palbociclib, an inhibitor of cyclin-dependent kinases (CDK) 4 and 6, significantly improved progression-free survival when administered as a first-line treatment in patients with hormone receptor-positive, metastatic ...
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This was the first clinical trial initiated to explore the hypothesis that activation of the HER pathway during tamoxifen treatment in ER-positive tumors contributes to acquired resistance. It was further hypothesized that simultaneous blockade of HER receptors and ER may delay this resistance even in tumors with low initial levels of EGFR/HER2 because expression of these proteins can increase when ER is blocked. The EGFR inhibitor gefitinib was chosen because it inhibits signaling from EGFR homo- and heterodimers and because it was effective in preclinical studies in which upregulation of EGFR was a dominant characteristic of tamoxifen-resistant tumors (16-18, 20, 21).. This randomized phase II trial was not designed to show a statistically significant advantage for the addition of gefitinib to tamoxifen, but rather to determine whether the addition of gefitinib resulted in a numerical advantage compared with placebo of sufficient interest to warrant further study. This proof-of-concept trial ...
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1,2,4-Triazole-Based N-Heterocyclic Carbene Nickel Complexes - Synthesis and Catalytic Application: Four nickel complexes bearing 1,2,4-triazole-based N-heteroc
Treatment with the aromatase inhibitor letrozole (Femara) can reduce the risk of breast cancer recurrence even when initiated one to seven years after a course of tamoxifen therapy. The results of a study involving women originally in the placebo arm of an international trial of letrozole will appear in the Journal of Clinical Oncology and are receiving early online release. Among those who chose to begin letrozole treatment after the initial trial was halted, the risk that their cancer would recur was cut in half compared with those who never received letrozole. In addition, the risk of metastasis was 60 percent lower with letrozole, and the chance that a new tumor would develop in the unaffected breast dropped more than 80 percent.
Letrozole Femara Powder Product Name:Letrozole Key words:Letrozole,Letrozole,Letrozole,Letrozole,Femara,Femara,Femara Alias:Femara CAS No.:112809-51-5 Molecular Formula:C17H11N5 Molecular Weight:285.3 Purity:99% Appearance:White power . Use:pharmaceutical intermediates, after menopause advanced breast cancer, - Letrozole Femara Powder Details.
In a randomized, Phase III trial led by researchers at The University of Texas MD Anderson Cancer Center, ribociclib, in combination with the aromatase inhibitor letrozole, dramatically improved progression-free survival (PFS) of post-menopausal women with hormone receptor-positive metastatic breast cancer, compared to the hormone therapy alone.
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In this application note we present the enantiomeric and/or diastereomeric resolutions of 12 triazole fungicides using Trefoil Column Technology.
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This study compared the efficacy, tolerability and quality-of-life (QoL) effects of adjuvant anastrozole then letrozole versus letrozole then anastrozole in
The exact meaning of the medical terminology,Carboxyamidotriazole - An anticancer drug that belongs to the family of drugs called angiogenesis inhibitors, is clearly explained in Medindia s glossary of medical terms
Authors: MEVLUT SERDAR, NURHAN GÜMRÜKÇÜOĞLU, ŞENGÜL ALPAY KARAOĞLU, NESLİHAN DEMİRBAŞ Abstract: A series of acylhydrazones (2a-d) was synthesized from the reactions of iminoester hydrochlorides (1a-e) with acyl hydrazines. 2,5-Dialkyl 1,3,4-oxadiazoles (3a-d) were obtained in the same reaction media. The treatment of acylhydrazones with hydrazine hydrate afforded 4-amino-3,5-dialkyl-1,2,4-triazoles (4a-c). The acetylation of 4-amino-3-(4-hydroxyphenyl)-5-phenyl-4H-1,2,4-triazole (4a) produced 4-amino-5-(4-acetoxyphenyl)-3-phenyl-4H-1,2,4-triazole (9), while the acetylation of 4-amino-3-(4-tolyl)-5-phenyl-4H-1,2,4-triazole (4b) gave 4-acetylamino-3-phenyl-5-(4-tolyl)-4H-1,2,4-triazole (10). The treatment of compound 4b with various aromatic aldehydes or acetophenone and 4-nitroacetophenone resulted in the formation of 4-arylidenamino-3,5-dialkyl-4H-1,2,4-triazoles (5a-e and 7a,b). Sodium borohydride reduction of 4-arylidenamino derivatives of 1,2,4-triazoles afforded ...
A class of oral drugs for treating breast cancer known as cyclin-dependent kinase (CDK) 4/6 inhibitors are generally well-tolerated, with a manageable toxicity profile for most patients. This is the conclusion of a comprehensive review of toxicities and drug interactions related to this class of drugs, published by Spring et al in The Oncologist.. The excitement surrounding CDK4/6 inhibitors is due to their potential for treating hormone receptor-positive metastatic breast cancer, the most common form of the disease. The first CDK4/6 inhibitors were recently approved by the U.S. Food and Drug Administration (FDA), with palbociclib (Ibrance) approved in February 2015 and ribociclib (Kisqali) approved in March 2017. A third, abemaciclib, is currently undergoing phase III trials. All three CDK4/6 inhibitors have received Breakthrough Therapy designation from the FDA.. CDK inhibitors have changed the landscape of management of hormone receptor-positive breast cancer, said Aditya Bardia, MBBS, MPH, ...
Although there was less toxicity, neoadjuvant letrozole plus palbociclib had similar response and BCS rates when compared with chemotherapy.
Effects of Hexaconazole on Growth and Antioxidant Potential of Cucumber Seedlings under UV-B Radiation - Antioxidative enzymes;Cucumber;Hexaconazole;Photosynthetic pigments;UV-B;
The posaconazole prescribing information recommends an upfront cyclosporine dosage reduction upon initiation of posaconazole prophylaxis. recommendation might be modified. TEXT Posaconazole is certainly a book triazole with broad-spectrum antifungal activity and a good toxicity profile (4 7 thats currently accepted for principal antifungal prophylaxis in allogeneic bloodstream and marrow transplantation (allo-BMT) recipients with graft-versus-host disease (GVHD) (18). Posaconazole prophylaxis in allo-BMT recipients is generally administered in combination with immunosuppressive drugs for GVHD Wortmannin prophylaxis and/or treatment most commonly cyclosporine (CsA). On the basis of its CYP3A4-inhibitory activity posaconazole increases the exposure to CsA warranting a recommendation for close monitoring. ...
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Five new metal-organic coordination polymers ([Cu{sub 3}(μ{sub 2}-OH){sub 2}(atrz){sub 2}(nph){sub 2}(H{sub 2}O){sub 2}]·2H{sub 2}O){sub n} (1), ([Cu{sub 2}(μ{sub 3}-OH)(atrz)(1,2,4-btc)]·2H{sub 2}O){sub n} (2), ([Cu{sub 2}(μ{sub 3}-OH)(atrz)(1,2,4-btc)(H{sub 2}O)]·H{sub 2}O){sub n} (3), [Cu(dth){sub 0.5}(nph)(H{sub 2}O)]{sub n} (4) and [Cu(dth)(Hnip){sub 2}]{sub n} (5) [atrz=4-amino-1,2,4-triazole, dth=N,N-di(4H-1,2,4-triazole)hexanamide, H{sub 2}nph=3-nitrophthalic acid, 1,2,4-H{sub 3}btc=1,2,4-benzenetricarboxylic acid and H{sub 2}nip=5-nitroisophthalic acid] were hydrothermally synthesized and structurally characterized. Polymer 1 shows a one-dimensional (1D) chain. Polymers 2 and 3 exhibit similar tetranuclear Cu{sup II}{sub 4} cluster-based three-dimensional (3D) frameworks with the same components. Polymer 4 possesses a 3D framework with a 4{sup 12}·6{sup 3}-pcu topology. Polymer 5 displays a 3D framework with a 4{sup 4}·6{sup 10}·8-mab topology. The magnetic properties of 1-4 ...
Voriconazole is an antifungal agent which has been approved for treatment of a broad range of fungal infections, including those caused by Candida species. The authors, from the United Kingdom, the United States of America and New Zealand, analyzed susceptibility data for the yeasts isolated from patients taking part in the voriconazole phase III clinical trials. The aim was to compare the effectiveness of voriconazole with other agents, by studying the yeasts response to these antifungal agents in vitro, and also to check for resistance to voriconazole. The researchers analyzed the effect of itraconazole, fluconazole, amphotericin B and voriconazole versus 1763 yeasts isolated from samples obtained from 472 patients. The yeast cultures obtained were predominantly Candida spp. (97.1%), although there were seven genera and 22 species of yeasts in all. The infections the patients were suffering from arose most commonly from surgery/trauma/burns (37% of patients), haematological malignancy (13%) ...
Letz from Chemech, Letrozole - Anolet to Oncolet | Letrozole is an oral non-steroidal aromatase inhibitor for the treatment of hormonally-responsive breast cancer after surgery. Use of Letz from Chemech, Pregnancy, lactation in childrens and special precautions for Letz from Chemech, prices of Letz from Chemech . Estrogens are produced by the conversion of androgens through the activity of the aromatase enzyme. Estrogens then bind to an estrogen receptor, which causes cells to divide. Letrozole prevents the aromatase from producing estrogens by competitive, reversible binding to the heme of its cytochrome P450 unit. The action is specific, and letrozole does not reduce production of mineralo- or corticosteroids.In contrast, tamoxifen interferes with the estrogen receptor. Tamoxifen is also used to treat hormonally- responsive breast cancer. However, letrozole is effective only in post-menopausal women, in whom estrogen is produced predominantly by the adrenal glands. In pre-menopausal women, estrogen is
Background:. Invasive fungal infections cause significant mortality and morbidity. Isavuconazole (ISV) is a new triazole approved for treatment of mucormycosis and aspergillosis. Data on its effectiveness outside clinical trials and in patients receiving prior triazole prophylaxis are lacking. Methods:. We conducted a retrospective cohort study on all patients at the Cleveland Clinic 6/1/2015 1/31/2017 who received ISV to determine 6-week response in a population with varying underlying diseases, and previous triazole prophylaxis or treatment. Descriptive statistics and univariate associations were calculated. Results:. 33 patients were identified including Organ transplant recipients (5), Hematopoietic cell transplant recipients (7), and acute leukemia (18). 25 had lung involvement while 13 had rhino-orbital-cerebral disease. In 13 cases, a fungal pathogen was identified: Mucorales (7) and Aspergillus (6). 15 received triazole prophylaxis prior to initiating ISV. 24 received antifungal therapy ...
There is increasing evidence that the use of chemicals frequently results in widespread environmental contamination with little understanding of the toxicological implications. Benzotriazoles are used in, among other applications, dishwashing formulations for home use, and are a class of chemicals recently reported to be present in European waters. This study demonstrates their presence in UK wastewaters, rivers, and drinking water. It also estimates that their use as silver polishing agents in dishwasher tablets and powders may account for a significant proportion of inputs to wastewaters. The lack of a complete set of good quality (eco)toxicological data on possible chronic effects of these high use chemicals should caution against using them in a manner which may have contributed to such widespread environmental contamination.. ...
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X] Isavuconazole (ISZ) is a newly available broad-spectrum triazole agent recently approved for the treatment of both invasive aspergillosis and mucormycosis. The aim of this study was to develop a simple and reliable method for therapeutic drug monitoring (TDM) of ISZ in human plasma samples. The method involves using a kit from ChromSystems intended for TDM of itraconazole (ITZ), posaconazole (PSZ), and voriconazole (VRZ) in serum/plasma for sample preparation and high-performance liquid chromatography, using fluorescence detection with emission and excitation wavelengths set to 261 and 366 nm, respectively. The assay was linear over the ISZ concentration range of 0.2 to 20.0 mg/liter, using a 0.1-ml sample volume. The inter- and intraday coefficients of variation were all below 3.7%, whereas the accuracies ranged from 95.0 to 106.2% and the mean extraction recovery was 91.9%. In addition, the method worked well using four different Vacutainer types, with six different healthy volunteers and ...
0385] In another embodiment, the invention relates to compounds selected from the group consisting of: [0386] 1-(3,4,5-trimethoxy-phenyl)-5-(4-bromo-phenyl)-1H-[1,2,3]triazole; [0387] 1-(2-hydroxy-4-methoxy-5-ethyl-phenyl)-5-(naphthylen-2-yl)-1H-[1,2,3]tria- zole; [0388] 1-(3,4,5-trimethoxy-phenyl)-5-(4-methoxy-phenyl)-1H-[1,2,3]triazole; [0389] 1-(2-hydroxy-4-methoxy-5-ethyl-phenyl)-5-(4-iodo-phenyl)-1H-[1,2,3- ]triazole; [0390] 1-(3,4,5-trimethoxy-phenyl)-5-[4-(N,N-dimethylamino)-phenyl]-1H-[1,2,3]tr- iazole; [0391] 1-(2-hydroxy-4-methoxy-5-ethyl-phenyl)-5-(4-bromo-phenyl)-1H-[1,2,3]triaz- ole; [0392] 1-(2-hydroxy-4-methoxy-5-(2,3-dihydro-benzo[1,4]dioxin-6-yl)-5-(4-bromo-p- henyl)-1H-[1,2,3]triazole; [0393] 1-(3,4,5-hydroxy-phenyl)-5-(4-hyoxy-phenyl)-1H-[1,2,3]triazole; [0394] 1-(3,4,5-trimethoxy-phenyl)-5-(4-iodo-phenyl)-1H-[1,2,3]triazole; [0395] 1-(3,4,5-trimethoxy-phenyl)-5-(3-fluoro-4-methoxy-phenyl)-1H-[1,2,3]triaz- ole; [0396] ...
Abstract. Structured peptides have gained more attention over time because of their biol. properties, biocompatibility and ability to act as modulators of protein/protein interactions, antibiotics, analgesics, immunosuppressants, and imaging agents to cite a few relevant applications. However, their poor bioavalability due in part to the susceptibility of the peptide bond to proteolytic cleavages has often impaired their development and considerably limited their therapeutic use. To circumvent these problems, many efforts have been undertaken to discover stable amide bond mimics resistant to proteolytic degrdn. Among them the 1,2,3-triazole (Tz) moiety has emerged as a highly stable analog of the trans-peptide bond as a means of generating bioactive peptides. Here we report a convenient approach to readily substitute amide bonds by triazole rings in Aib-contg. peptides using Aibψ[Tz]-Xaa dipeptide-like units. We have defined their application in solid phase synthesis and generated short model ...
The pharmacokinetics of orally administered solithromycin in healthy subjects have recently been reported (17). Following escalating single doses (50 to 1,600 mg), Cmax and measurements of AUC increased in a greater-than-dose-proportional manner up to 1,200 mg. The mean elimination half-life also increased from 3.16 to 7.42 h over the dosing range evaluated. Administration of a high-fat meal was shown to not affect the oral bioavailability of solithromycin. Moderate amounts of accumulation (1.7 to 2.2 times greater on day 7 than on day 1) were observed after multiple daily doses (200, 400, and 600 mg).. The observed plasma concentrations in our study are similar to those obtained with 400 mg in the multiple-oral-dose pharmacokinetic study of solithromycin (17). The mean (± SD) plasma Cmax of solithromycin in that study was 1.09 ± 0.52 mg/liter (at a mean Tmax of 4.00 h), whereas our observed Cmax was 0.90 ± 0.46 mg/liter (at a mean Tmax of 3.57 h). Similarly, the reported trough plasma ...
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Lee S. Schwartzberg, MD, of the West Cancer Center, discusses phase III results from the CONTESSA study, which showed that an all-oral regimen of tesetaxel plus a reduced dose of capecitabine significantly improved progression-free survival compared with capecitabine alone in patients with HER2-negative, hormone receptor-positive metastatic breast cancer previously treated with a taxane (Abstract GS4-01).. Editors note: On March 22, 2021, Odonate Therapeutics announced it was discontinuing the development of tesetaxel and will close the companys operations. Read more here.. ...
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Herein, we assessed the characteristics of AZD5153, a novel BET bromodomain inhibitor. The bivalent binding mode of AZD5153 sets it apart from previously described BET bromodomain inhibitors. Mechanistically, the simultaneous ligation of both BRD4 bromodomains by AZD5153 allows for efficient displacement of BRD4 from chromatin at lower drug concentrations. This unique biophysical property translates into enhanced in vitro and in vivo pharmacologic activity.. In the hematologic tumor setting, our comparative efficacy studies with QD, BID, and continuous dosing of AZD5153 have revealed that duration of target coverage is the primary driver for in vivo efficacy. Twice-daily dosing with the split QD dose mitigated the issue of fast clearance of AZD5153 from the mouse system and provided longer duration of target inhibition translating into better efficacy. We enhanced these findings by using mini-pump drug infusion, which eliminates PK fluctuations and provides consistent target inhibition. Compared ...