A non-selective post-emergence, translocated herbicide. According to the Seventh Annual Report on Carcinogens (PB95-109781, 1994) this substance may reasonably be anticipated to be a carcinogen. (From Merck Index, 12th ed) It is an irreversible inhibitor of CATALASE, and thus impairs activity of peroxisomes.
Organic chemistry methodology that mimics the modular nature of various biosynthetic processes. It uses highly reliable and selective reactions designed to "click" i.e., rapidly join small modular units together in high yield, without offensive byproducts. In combination with COMBINATORIAL CHEMISTRY TECHNIQUES, it is used for the synthesis of new compounds and combinatorial libraries.
Substances that destroy fungi by suppressing their ability to grow or reproduce. They differ from FUNGICIDES, INDUSTRIAL because they defend against fungi present in human or animal tissues.
A triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes required for ERGOSTEROL synthesis.
Hydrocarbons with at least one triple bond in the linear portion, of the general formula Cn-H2n-2.
Chemicals that kill or inhibit the growth of fungi in agricultural applications, on wood, plastics, or other materials, in swimming pools, etc.
Triazole antifungal agent that is used to treat oropharyngeal CANDIDIASIS and cryptococcal MENINGITIS in AIDS.
The ability of fungi to resist or to become tolerant to chemotherapeutic agents, antifungal agents, or antibiotics. This resistance may be acquired through gene mutation.
Infections with fungi of the genus ASPERGILLUS.
A species of imperfect fungi from which the antibiotic fumigatin is obtained. Its spores may cause respiratory infection in birds and mammals.
A family of 6-membered heterocyclic compounds occurring in nature in a wide variety of forms. They include several nucleic acid constituents (CYTOSINE; THYMINE; and URACIL) and form the basic structure of the barbiturates.
Any tests that demonstrate the relative efficacy of different chemotherapeutic agents against specific microorganisms (i.e., bacteria, fungi, viruses).
Organic or inorganic compounds that contain the -N3 group.
A genus of yeast-like mitosporic Saccharomycetales fungi characterized by producing yeast cells, mycelia, pseudomycelia, and blastophores. It is commonly part of the normal flora of the skin, mouth, intestinal tract, and vagina, but can cause a variety of infections, including CANDIDIASIS; ONYCHOMYCOSIS; vulvovaginal candidiasis (CANDIDIASIS, VULVOVAGINAL), and thrush (see CANDIDIASIS, ORAL). (From Dorland, 28th ed)
Rhodium. A hard and rare metal of the platinum group, atomic number 45, atomic weight 102.905, symbol Rh. (Dorland, 28th ed)
Infection with a fungus of the genus CANDIDA. It is usually a superficial infection of the moist areas of the body and is generally caused by CANDIDA ALBICANS. (Dorland, 27th ed)
The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds.
Macrolide antifungal antibiotic produced by Streptomyces nodosus obtained from soil of the Orinoco river region of Venezuela.
Changing an open-chain hydrocarbon to a closed ring. (McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)
A genus of mitosporic fungi containing about 100 species and eleven different teleomorphs in the family Trichocomaceae.
Compounds that specifically inhibit STEROL 14-DEMETHYLASE. A variety of azole-derived ANTIFUNGAL AGENTS act through this mechanism.
Five membered rings containing a NITROGEN atom.
Cyclic hexapeptides of proline-ornithine-threonine-proline-threonine-serine. The cyclization with a single non-peptide bond can lead them to be incorrectly called DEPSIPEPTIDES, but the echinocandins lack ester links. Antifungal activity is via inhibition of 1,3-beta-glucan synthase production of BETA-GLUCANS.
The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)
Infections of the respiratory tract with fungi of the genus ASPERGILLUS. Infections may result in allergic reaction (ALLERGIC BRONCHOPULMONARY ASPERGILLOSIS), colonization in pulmonary cavities as fungus balls (MYCETOMA), or lead to invasion of the lung parenchyma (INVASIVE PULMONARY ASPERGILLOSIS).
A kingdom of eukaryotic, heterotrophic organisms that live parasitically as saprobes, including MUSHROOMS; YEASTS; smuts, molds, etc. They reproduce either sexually or asexually, and have life cycles that range from simple to complex. Filamentous fungi, commonly known as molds, refer to those that grow as multicellular colonies.
Synthetic organic reactions that use reactions between unsaturated molecules to form cyclical products.
Broad spectrum antifungal agent used for long periods at high doses, especially in immunosuppressed patients.
A fungal infection that may appear in two forms: 1, a primary lesion characterized by the formation of a small cutaneous nodule and small nodules along the lymphatics that may heal within several months; and 2, chronic granulomatous lesions characterized by thick crusts, warty growths, and unusual vascularity and infection in the middle or upper lobes of the lung.
Organic compounds containing the -CN radical. The concept is distinguished from CYANIDES, which denotes inorganic salts of HYDROGEN CYANIDE.
A mitosporic fungal genus previously called Monosporium. Teleomorphs include PSEUDALLESCHERIA.
A steroid of interest both because its biosynthesis in FUNGI is a target of ANTIFUNGAL AGENTS, notably AZOLES, and because when it is present in SKIN of animals, ULTRAVIOLET RAYS break a bond to result in ERGOCALCIFEROL.
A mitosporic fungal genus causing opportunistic infections, endocarditis, fungemia, a hypersensitivity pneumonitis (see TRICHOSPORONOSIS) and white PIEDRA.
An oxidoreductase that catalyzes the conversion of HYDROGEN PEROXIDE to water and oxygen. It is present in many animal cells. A deficiency of this enzyme results in ACATALASIA.
Lung infections with the invasive forms of ASPERGILLUS, usually after surgery, transplantation, prolonged NEUTROPENIA or treatment with high-doses of CORTICOSTEROIDS. Invasive pulmonary aspergillosis can progress to CHRONIC NECROTIZING PULMONARY ASPERGILLOSIS or hematogenous spread to other organs.
Elements with partially filled d orbitals. They constitute groups 3-12 of the periodic table of elements.
A technology, in which sets of reactions for solution or solid-phase synthesis, is used to create molecular libraries for analysis of compounds on a large scale.
The facilitation of a chemical reaction by material (catalyst) that is not consumed by the reaction.
The ability of fungi to resist or to become tolerant to several structurally and functionally distinct drugs simultaneously. This resistance phenotype may be attributed to multiple gene mutations.
A unicellular budding fungus which is the principal pathogenic species causing CANDIDIASIS (moniliasis).
A species of MITOSPORIC FUNGI that is a major cause of SEPTICEMIA and disseminated CANDIDIASIS, especially in patients with LYMPHOMA; LEUKEMIA; and DIABETES MELLITUS. It is also found as part of the normal human mucocutaneous flora.
Infection with a fungus of the genus COCCIDIOIDES, endemic to the SOUTHWESTERN UNITED STATES. It is sometimes called valley fever but should not be confused with RIFT VALLEY FEVER. Infection is caused by inhalation of airborne, fungal particles known as arthroconidia, a form of FUNGAL SPORES. A primary form is an acute, benign, self-limited respiratory infection. A secondary form is a virulent, severe, chronic, progressive granulomatous disease with systemic involvement. It can be detected by use of COCCIDIOIDIN.
A non-taxonomic term for unicellular microscopic algae which are found in both freshwater and marine environments. Some authors consider DIATOMS; CYANOBACTERIA; HAPTOPHYTA; and DINOFLAGELLATES as part of microalgae, even though they are not algae.
Any of the monobasic inorganic or organic acids of sulfur with the general formula RSO(OH). (From McGraw Hill Dictionary of Scientific and Technical Terms, 4th ed)
Methods used for the chemical synthesis of compounds. Included under this heading are laboratory methods used to synthesize a variety of chemicals and drugs.
The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.
Inflammation of the periosteum. The condition is generally chronic, and is marked by tenderness and swelling of the bone and an aching pain. Acute periostitis is due to infection, is characterized by diffuse suppuration, severe pain, and constitutional symptoms, and usually results in necrosis. (Dorland, 27th ed)
Ring compounds having atoms other than carbon in their nuclei. (Grant & Hackh's Chemical Dictionary, 5th ed)
An irregularly shaped cavity in the RHOMBENCEPHALON, located between the MEDULLA OBLONGATA; the PONS; and the isthmus in front, and the CEREBELLUM behind. It is continuous with the central canal of the cord below and with the CEREBRAL AQUEDUCT above, and through its lateral and median apertures it communicates with the SUBARACHNOID SPACE.
An NADPH-dependent P450 enzyme that plays an essential role in the sterol biosynthetic pathway by catalyzing the demethylation of 14-methyl sterols such as lanosterol. The enzyme acts via the repeated hydroxylation of the 14-methyl group, resulting in its stepwise conversion into an alcohol, an aldehyde and then a carboxylate, which is removed as formic acid. Sterol 14-demethylase is an unusual cytochrome P450 enzyme in that it is found in a broad variety of organisms including ANIMALS; PLANTS; FUNGI; and protozoa.
A species of MITOSPORIC FUNGI commonly found on the body surface. It causes opportunistic infections especially in immunocompromised patients.
A heavy metal trace element with the atomic symbol Cu, atomic number 29, and atomic weight 63.55.
Compounds consisting of a short peptide chain conjugated with an acyl chain.
Agents destructive to the protozoal organisms belonging to the suborder TRYPANOSOMATINA.
Pulmonary diseases caused by fungal infections, usually through hematogenous spread.
A fluorinated cytosine analog that is used as an antifungal agent.
Infection resulting from inhalation or ingestion of spores of the fungus of the genus HISTOPLASMA, species H. capsulatum. It is worldwide in distribution and particularly common in the midwestern United States. (From Dorland, 27th ed)
A species of the fungus CRYPTOCOCCUS. Its teleomorph is Filobasidiella neoformans.
Peptides whose amino and carboxy ends are linked together with a peptide bond forming a circular chain. Some of them are ANTI-INFECTIVE AGENTS. Some of them are biosynthesized non-ribosomally (PEPTIDE BIOSYNTHESIS, NON-RIBOSOMAL).
A superfamily of hundreds of closely related HEMEPROTEINS found throughout the phylogenetic spectrum, from animals, plants, fungi, to bacteria. They include numerous complex monooxygenases (MIXED FUNCTION OXYGENASES). In animals, these P-450 enzymes serve two major functions: (1) biosynthesis of steroids, fatty acids, and bile acids; (2) metabolism of endogenous and a wide variety of exogenous substrates, such as toxins and drugs (BIOTRANSFORMATION). They are classified, according to their sequence similarities rather than functions, into CYP gene families (>40% homology) and subfamilies (>59% homology). For example, enzymes from the CYP1, CYP2, and CYP3 gene families are responsible for most drug metabolism.
Infection with a fungus of the species CRYPTOCOCCUS NEOFORMANS.

Interleukin-12 is synthesized by mesangial cells and stimulates platelet-activating factor synthesis, cytoskeletal reorganization, and cell shape change. (1/3718)

Preliminary studies indicate the involvement of interleukin (IL)-12 in experimental renal pathology. In the present study, we evaluated whether cultured glomerular mesangial cells are able to produce IL-12 and whether IL-12 may regulate some of their functions, including the cytoskeletal reorganization, the change in cell shape, and the production of platelet-activating factor (PAF). The results obtained indicate that pro-inflammatory stimuli, such as tumor necrosis factor-alpha and bacterial polysaccharides, induce the expression of IL-12 mRNA and the synthesis of the protein by cultured mesangial cells. Moreover, cultured mesangial cells were shown to bind IL-12 and to express the human low-affinity IL-12 beta1-chain receptor. When challenged with IL-12, mesangial cells produced PAF in a dose- and time-dependent manner and superoxide anions. No production of tumor necrosis factor-alpha and IL-8 was observed. Moreover, we demonstrate that IL-12 induced a delayed and sustained shape change of mesangial cells that reached its maximum between 90 and 120 minutes of incubation. The changes in cell shape occurred concomitantly with cytoskeletal rearrangements and may be consistent with cell contraction. As IL-12-dependent shape change of mesangial cells was concomitant with the synthesis of PAF, which is known to promote mesangial cell contraction, we investigated the role of PAF using two chemically different PAF receptor antagonists. Both antagonists inhibited almost completely the cell shape change induced by IL-12, whereas they were ineffective on angiotensin-II-induced cell shape change. In conclusion, our results suggest that mesangial cells can either produce IL-12 or be stimulated by this cytokine to synthesize PAF and to undergo shape changes compatible with cell contraction.  (+info)

Systemic candidiasis with candida vasculitis due to Candida kruzei in a patient with acute myeloid leukaemia. (2/3718)

Candida kruzei-related systemic infections are increasing in frequency, particularly in patients receiving prophylaxis with antifungal triazoles. A Caucasian male with newly diagnosed acute myeloid leukaemia (AML M1) developed severe and persistent fever associated with a micropustular eruption scattered over the trunk and limbs during induction chemotherapy. Blood cultures grew Candida kruzei, and biopsies of the skin lesions revealed a candida vasculitis. He responded to high doses of liposomal amphotericin B and was discharged well from hospital.  (+info)

Glutamate receptor signaling interplay modulates stress-sensitive mitogen-activated protein kinases and neuronal cell death. (3/3718)

Glutamate receptors modulate multiple signaling pathways, several of which involve mitogen-activated protein (MAP) kinases, with subsequent physiological or pathological consequences. Here we report that stimulation of the N-methyl-D-aspartate (NMDA) receptor, using platelet-activating factor (PAF) as a messenger, activates MAP kinases, including c-Jun NH2-terminal kinase, p38, and extracellular signal-regulated kinase, in primary cultures of hippocampal neurons. Activation of the metabotropic glutamate receptor (mGluR) blocks this NMDA-signaling through PAF and MAP kinases, and the resultant cell death. Recombinant PAF-acetylhydrolase degrades PAF generated by NMDA-receptor activation; the hetrazepine BN50730 (an intracellular PAF receptor antagonist) also inhibits both NMDA-stimulated MAP kinases and neuronal cell death. The finding that the NMDA receptor-PAF-MAP kinase signaling pathway is attenuated by mGluR activation highlights the exquisite interplay between glutamate receptors in the decision making process between neuronal survival and death.  (+info)

Treatment of murine fusariosis with SCH 56592. (4/3718)

Doses of 10 to 100 mg of the azole antifungal agent SCH 5692/kg of body weight/day were studied in immunocompetent mice as therapy for systemic infection by Fusarium solani. Treatment was begun 1 h after intravenous infection and continued daily for 4 or 13 doses. Prolongation of survival and organ clearance were dependent on both the dose and the duration of SCH 56592 therapy, with the best results seen at 50 and 100 mg/kg/day. The results at the highest doses of SCH 56592 used (50 or 100 mg/kg/day) were comparable to those obtained with amphotericin B at 1 mg/kg/day. SCH 56592 has potential for therapy of systemic infections caused by F. solani.  (+info)

Postnatal development of hippocampal dentate granule cell gamma-aminobutyric acidA receptor pharmacological properties. (5/3718)

Postnatal development of hippocampal dentate granule cell gamma-aminobutyric acidA (GABAA) receptor pharmacological properties was studied. Granule cells were acutely isolated from hippocampi of 7- to 14- and 45- to 52-day-old rats, and whole cell patch-clamp recordings were obtained. The sensitivity of GABAA receptors to GABA and modulation of GABAA receptor currents by benzodiazepines (BZ), zinc, furosemide, and loreclezole was studied. Multiple changes in the pharmacological properties of dentate granule-cell GABAA receptors occurred during the first 52 days of postnatal development: GABA-evoked maximal current increased with postnatal age; GABAA receptors changed from BZ type 3 in young rats to BZ type 1 in adult rats; furosemide and zinc inhibited GABAA receptor currents in young rats but not in adult rats; the fraction of cells that expressed loreclezole-sensitive GABAA receptors increased with postnatal age. These findings suggest that dentate granule cells in young and adult animals express pharmacologically distinct GABAA receptors and that the postnatal development of these receptors is prolonged, lasting at least 45 days. Comparison with the previously reported pharmacological properties of GABAA receptors on dentate granule cells acutely isolated from hippocampi of 28- to 35-day-old rats suggests that receptors expressed at that age have properties intermediate between young and adult rats.  (+info)

In-vitro activity of voriconazole, itraconazole and amphotericin B against filamentous fungi. (6/3718)

The in-vitro fungistatic and fungicidal activities of voriconazole were compared with those of itraconazole and amphotericin B. MICs for 110 isolates belonging to 11 species of filamentous fungi were determined by a broth microdilution adaptation of the method recommended by the National Committee for Clinical Laboratory Standards. Minimum lethal concentrations (MLCs) of the three antifungal agents were also determined. The MIC ranges of the three compounds were comparable for Aspergillus flavus, Aspergillus fumigatus, Cladophialophora bantiana and Exophiala dermatitidis. Voriconazole and itraconazole were more active than amphotericin B against Fonsecaea pedrosoi, but the two azole agents were less active against Sporothrix schenckii. Voriconazole was more active than itraconazole or amphotericin B against Scedosporium apiospermum, but less active than the other two agents against two mucoraceous moulds, Absidia corymbifera and Rhizopus arrhizus. Voriconazole and amphotericin B were more active than itraconazole against Fusarium solani. With the exception of S. apiospermum, all the moulds tested had MLC50 values of < or =2 mg/L and MLC90 values of < or =4 mg/L against amphotericin B. Voriconazole and itraconazole showed fungicidal effects against five of the 1 1 moulds tested (A. flavus, A. fumigatus, C. bantiana, E. dermatitidis and F. pedrosoi) with MLC90 values of < or =2 mg/L. In addition, voriconazole was fungicidal for Phialophora parasitica. Our results suggest that voriconazole could be effective against a wide range of mould infections in humans.  (+info)

Effect of DL111-IT on progesterone biosynthesis and viability of rat luteal cells in vitro. (7/3718)

AIM: To study the influence of DL111-IT on progesterone biosynthesis of cultured luteal cells (LC). METHODS: LC viability was assessed with trypan blue dye exclusion and progesterone concentration was measured with radioimmunoassay. RESULTS: DL111-IT decreased the viability of LC after 24-h incubation, its ED50 being 7.7 (95% confidence limits: 7.1-8.5) mg.L-1. DL111-IT inhibited basal secretion of progesterone in a concentration-dependent manner, and 3 mg.L-1 decreased progesterone concentration by 25% vs control. DL111-IT 3 mg.L-1 also inhibited the stimulatory effect of forskolin (cAMP activator) 10 mumol.L-1 and pregnenolone [converted to progesterone by 3 beta-hydroxysteroid dehydrogenase-isomerase complex (3 beta-HSD)] 10 mumol.L-1 on progesterone production in cultured LC, and their inhibitory rates were 43% and 155%, respectively. At the same concentration, DL111-IT did not influence hCG-induced progesterone production. CONCLUSION: DL111-IT inhibited progesterone synthesis by suppressing the conversion of pregnenolone to progesterone (inactivating 3 beta-HSD) and suppressed the activity of cAMP. DL111-IT 6-24 mg.L-1 decreased the viability of LC.  (+info)

2-mercapto N-(azolyl)benzenesulfonamides. VI. Synthesis and anti-HIV activity of some new 2-mercapto-N-(1,2,4-triazol-3-yl)benzenesulfonamide derivatives containing the 1,2,4-triazole moiety fused with a variety of heteroaromatic rings. (8/3718)

A series of 2-mercapto-N-(1,2,4-triazol-3-yl)benzenesulfonamide derivatives containing the triazole moiety fused with a variety of heteroaromatic rings [XVI-XXVIII] was obtained by the reactions of 3-methylthio-1,4-2-benzodithiazine 1,1-dioxide derivatives [Ia-d] with 2-hydrazines [IIa-f]. Some of the intermediate 1,1-dioxide-1,4,2-benzodithiazin-3-ylhydrazines [III-XV] initially formed were also isolated. Preliminary screening data indicated that compounds [XVI-XIX and XXVII] were anti-HIV inactive, whereas other compounds showed a high [XXI and XXIII], fairly high [XXIII and XXVI] or moderate [XX, XXIV, XXV and XXVIII] activity. The compound [XXI] exhibited also high activity against ten selected HIV mutants.  (+info)

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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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 ...
Arimidex Raw Anastrozole Pharmade AAS Raw Steroid Quality 99.9 Anastrozole, Arimidex, Anastrozole Arimidex, Oral Anastrozole Arimidex , Anastrozole Arimidex Steriod Powder Arimidex is an Aromatase inhibitor which is used to control estrogenic side...
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 ...
M. R. Atkinson, J. B. Polya (1954). "Triazoles. Part II. N-substitution of some 1 : 2 : 4-triazoles". Journal of the Chemical ... 4-triazole isomer. Triazoles have been found to have a number of real world applications as antibacterial agents.[citation ... Substituted 1,2,4-triazole have been prepared from diverse imides and hydrazines. In the case that the R groups of the imide ... In their research on the synthesis of 1,2,4-triazoles, Potts determined that the strongest acidic group attached to the side of ...
Triazole has been shown in laboratory studies to effectively control mycelial growth and provides local systemic protection. ... "Fungicides: Triazoles , Integrated Crop Management." Integrated Crop Management, November 9, 2006. http://www.ipm.iastate.edu/ ...
Triazoles. This disambiguation page lists articles associated with the title COMU. If an internal link led you here, you may ...
These consist of mancozeb, triazoles,[which?] tridemorph, and strobilurin.[which?] Mancozeb seems to be the most effective ...
Ast, Sandra; Rutledge, Peter J.; Todd, Matthew H. (2012). "Reversing the Triazole Topology in a Cyclam-Triazole-Dye Ligand ... "Chemical sensors that incorporate click-derived triazoles". Chemical Society Reviews. 40 (5): 2848-66. doi:10.1039/C0CS00143K. ... "Chemical sensors that incorporate click-derived triazoles". Chemical Society Reviews. 40 (5): 2848-2866. doi:10.1039/C0CS00143K ...
Generally, treatment is with triazoles, preferably itraconazole. A second choice is potassium iodide, either alone or combined ...
Non-carbon reagents also undergo cyclization, e.g. Azide alkyne Huisgen cycloaddition to give triazoles. Cycloaddition ...
C. Ainsworth (1960). "1,2,4-Triazole". Organic Syntheses. 40: 99. doi:10.15227/orgsyn.040.0099. (Articles without InChI source ... Formylation of thiosemicarbazide provides access to triazole. International Union of Pure and Applied Chemistry (2014). ...
"Europium confined cyclen dendrimers with photophysically active triazoles". Journal of Materials Chemistry. 18 (22): 2545. doi: ...
... s are poly-triazole-poly-peptide hybrid polymers. They are made of repeating units of a 1,2,3-triazole ... The triazole bridges do not confer any stability to oligopeptide. Degradation of the polymer occurs at the peptide bonds ... They can be visualized as an oligopeptide that is flanked at both the C-terminus and N-terminus by a triazole molecule. Clicked ... The molecules linked to one another by the azide-alkyne Huisgen cycloaddition are connected by an aromatic triazole which is ...
Sabo JA, Abdel-Rahman SM (September 2000). "Voriconazole: a new triazole antifungal". The Annals of Pharmacotherapy. 34 (9): ...
3-triazoles. An example of this reaction is shown below: The use of azides is very important in a variety of different ... triazoles". Synlett. 24: 41-44. doi:10.1055/s-0032-1317712. "Espacenet - Bibliographic data". Hein, C. D.; Liu, X. M.; Wang, D ...
Structurally, loreclezole is a triazole derivative. In animal seizure models, loreclezole is protective against ... Triazoles, GABAA receptor positive allosteric modulators, GABAA-rho receptor negative allosteric modulators, All stub articles ...
This set contains pyrrole, imidazole, pyrazole, triazoles, tetrazole, and pentazole. Substituted analogs of pentazole are ... Triazole, Tetrazole, and Pentazole Rings: Release of Parent Azoles. Generation of Unstable Pentazole, HN5/N5-, in Solution" ( ...
... , sold under the brand name Noxafil among others, is a triazole antifungal medication. It was approved for medical ... Rachwalski EJ, Wieczorkiewicz JT, Scheetz MH (October 2008). "Posaconazole: an oral triazole with an extended spectrum of ... Schiller DS, Fung HB (September 2007). "Posaconazole: an extended-spectrum triazole antifungal agent". Clinical Therapeutics. ...
Azole antifungals are generally divided into two groups, imidazoles and triazoles. Common examples of imidazoles include ... posaconazole and voriconazole fall under triazoles group. Both groups cause substantial damage in fungal membrane integrity by ...
However, a growing proportion of infections are resistant to the triazoles. A. fumigatus, the most commonly infecting species, ... May 2011). "High-frequency triazole resistance found In nonculturable Aspergillus fumigatus from lungs of patients with chronic ...
It is in the triazole family of medications. It works by affecting fungal metabolism and fungal cell membranes. Voriconazole ... Triazole antifungals, World Health Organization essential medicines). ...
It differs from earlier azole antifungals (such as ketoconazole) in that its structure contains a triazole ring instead of an ... While the imidazole antifungals are mainly used topically, fluconazole and certain other triazole antifungals are preferred ... Fluconazole is a first-generation triazole antifungal medication. ...
4-triazole; 1H- and 2H- isoindole. Ring-chain tautomers occur when the movement of the proton is accompanied by a change from ...
One example is the triazole antimycotics or fungicides. However, the chemical environments encountered en route from the ...
The resulting 1,2,3-triazole is fluorescent. The coumarin backbone is chosen to be used as the profluorophore due to its small ...
It is in the triazole family of medications. It stops fungal growth by affecting the cell membrane or affecting their ... Triazole antifungals, World Health Organization essential medicines, Phenylethanolamine ethers). ...
... sulfate, sold under the brand name Cresemba, is a systemic antifungal medication of the triazole class which is ... Guinea J, Bouza E (December 2008). "Isavuconazole: a new and promising antifungal triazole for the treatment of invasive fungal ... ISBN 978-1-284-17132-7. Miceli MH, Kauffman CA (November 2015). "Isavuconazole: A New Broad-Spectrum Triazole Antifungal Agent ... January 2003). "Design, synthesis and antifungal activity of a novel water soluble prodrug of antifungal triazole". Bioorganic ...
The chemical treatment with triazole fungicides is effective. There is no breeding program about rust tolerant plants designed ...
"A cycloaddition route to novel triazole boronic esters". Chem. Commun. (4): 436-438. doi:10.1039/b817052e. PMID 19137177. ...
Deferasirox is an N-substituted bis-hydroxyphenyl-triazole. It is capable of removing iron from the blood through the ...
It is the triazole analogue of Flunitrazepam (Rohypnol). The addition of the triazole ring to the scaffold increases potency ...
In the Einhorn-Brunner reaction hydrazines react with imides to give triazoles. Being a good nucleophile, N2H4 can attack ...
More chemicals include Triazoles an organosphosphate fungicide, Imazalil, Procholora and Fentin hydroxide. Registered ...
Learn why triazole-resistant aspergillosis is a prevention priority. ... People with a triazole-resistant infection have over a 30% higher likelihood of dying than patients with an infection that can ... Use of triazole fungicides in the environment increased more than fourfold from 2006 to 2016 in the United States, amplifying ... CDC has developed a plan to address the growing threat of triazole-resistant A. fumigatus and has begun the first phase of ...
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... the emergence of triazole-resistant A. fumigatus threatens the effectiveness of triazoles in clinical practice (3). Patients ... Patients can acquire triazole-resistant A. fumigatus infections because of exposure to long-term triazole therapy for chronic ... Fatal Fungicide-Associated Triazole-Resistant Aspergillus fumigatus Infection, Pennsylvania, USA On This Page ... Fatal Fungicide-Associated Triazole-Resistant Aspergillus fumigatus Infection, Pennsylvania, USA. Emerging Infectious Diseases ...
Catalyst-free facile synthesis of polycyclic indole/pyrrole substituted-1,2,3-triazoles J. Gour, S. Gatadi, R. Akunuri, M. V. ... Catalyst-free facile synthesis of polycyclic indole/pyrrole substituted-1,2,3-triazoles† ...
4-triazole (AMT) is used in the manufacture of the pesticide, flumetsulam. Analysis of AMT in biological fluids requires a ... The chemical, 3-amino-5-mercapto-1,2,4-triazole (AMT) is used in the manufacture of the pesticide, flumetsulam. Analysis of AMT ... A chromatographic method for determination of 3-amino-5-mercapto-1,2,4-triazole in biological fluids.. ...
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3 more authors) (2016) Towards Water Soluble Mitochondria-Targeting Theranostic Osmium(II) Triazole-Based Complexes. Molecules ...
Fifteen thiazolyl-triazole Schiff bases were evaluated for their antibacterial activity, measuring the growth inhibition zone ... Antibacterial Evaluation and Virtual Screening of New Thiazolyl-Triazole Schiff Bases as Potential DNA-Gyrase Inhibitors. ... The virtual screening concluded that thiazolyl-triazole Schiff base B8 is the best drug-like candidate, satisfying requirements ... Schiff bases, thiazole, and triazole derivatives are considered key scaffolds in medicinal chemistry. ...
4-triazole (Cat. No. 0564) has been withdrawn from sale for commercial reasons. ... 3-[(1-Methyl-4-nitro-1H-imidazol-5-yl)thio]-4-methyl-1,2,4-triazole. Cat. No. 0564 Submit a Review Datasheet / COA / SDS ... Have you used 3-[(1-Methyl-4-nitro-1H-imidazol-5-yl)thio]-4-methyl-1,2,4-triazole?. Submit a review and receive an Amazon gift ... Reviews for 3-[(1-Methyl-4-nitro-1H-imidazol-5-yl)thio]-4-methyl-1,2,4-triazole. There are currently no reviews for this ...
A boronate prochelator built on a triazole framework for peroxide-triggered tridentate metal binding. ... A boronate prochelator built on a triazole framework for peroxide-triggered tridentate metal binding. Journal Article (Journal ... We present here the synthesis and characterization of this triazole-based, self-immolative prochelator: TIP (4-(5-(2-((4- ...
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Dive into the research topics of Bis(trifluoromethyl)mercury(II) complexes with purine and 3,5-dimethyl-4 -amino-triazole as ... Bis(trifluoromethyl)mercury(II) complexes with purine and 3,5-dimethyl-4 -amino-triazole as ligands, [Hg(CF3)(2)(Pur)](4) and ... Bis(trifluoromethyl)mercury(II) complexes with purine and 3,5-dimethyl-4 -amino-triazole as ligands, [Hg(CF3)(2)(Pur)](4) and ... T1 - Bis(trifluoromethyl)mercury(II) complexes with purine and 3,5-dimethyl-4 -amino-triazole as ligands, [Hg(CF3)(2)(Pur)](4 ...
A number of known (1a - 3a, 7a - 9a, 1b - 3b, 7b, 9b) and novel (4a - 6a, 4b - 6b, 8b) 1-substituted- 4-phenyl-1,2,3-triazole ... The synthesis, characterization and preliminary biological evaluation of triazole complexes of palladium. dc.contributor. ... The synthesis, characterization and preliminary biological evaluation of triazole complexes of palladium. en_ZA. ... and 1-substituted-4-pyridyl-1,2,3-triazole ligands were synthesized, in moderate to good yields. The N-bound substituents were ...
4-triazole-3,5-diamine - cas 3310-68-7, synthesis, structure, density, melting point, boiling point ... Tags: melting point of N-phenyl-1H-1,2,4-triazole-3,5-diamine - 3310-68-7 , boiling point of N-phenyl-1H-1,2,4-triazole-3,5- ... diamine - 3310-68-7 , density of N-phenyl-1H-1,2,4-triazole-3,5-diamine - 3310-68-7 , refractive index of N-phenyl-1H-1,2,4- ...
These triazole-containing inhibitors exhibit sub-micromolar inhibition of the human isoform of GOAT (hGOAT), and provide a ... We report the first examples of GOAT inhibitors incorporating a triazole linkage as a biostable isosteric replacement for the ... A new class of ghrelin O-acyltransferase inhibitors incorporating triazole-linked lipid mimetic groups. ...
1,2,4-Triazole-3-thione compounds with a 4-ethyl alkyl/aryl sulfide substituent are broad-spectrum metallo-β-lactamase ... 1,2,4-Triazole-3-thione compounds with a 4-ethyl alkyl/aryl sulfide substituent are broad-spectrum metallo-β-lactamase ...
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Soil Biogeochemistry Group Seminar: Understanding the plant root uptake of [14C]-1,2,4-Triazole. 9 October 2019 @ 1:00 pm - 2: ...
Corrosion inhibition of 70Cu-30Zn alloy in 0,5 M HNO3 by 3-amino-1,2,4-triazole. S. El Issami1, L. Bazzi1, M. Mihit1, M. Hilali ... The inhibitive action of 3-amino-1,2,4-triazole (ATA) on 70Cu-30Zn alloy corrosion in HNO3 0,5M was examined. Gravimetric and ...
Pregnancy interceptive activity of triazoles, oxadiazoles & thiadiazoles.. Authors: Neelima,. Mehrotra, P K. Bhaduri, A P. ... Pregnancy interceptive activity of triazoles, oxadiazoles & thiadiazoles. Indian Journal of Medical Research. 1987 Aug; 86(): ...
Home New Study Fungicides Market size, share & trends analysis report by By Type (Chloronitriles, Dithiocarbamates, Triazoles, ... New Study Fungicides Market size, share & trends analysis report by By Type (Chloronitriles, Dithiocarbamates, Triazoles, ...
3-triazoles and efficient synthesis of suvorexant Org. Chem. Front., 2018, Advance Article DOI: 10.1039/C7QO00945C, Research ... A wide variety of aryl esters containing 1,2,3-triazoles were obtained in moderate to good yields. In addition, density ... Home » Uncategorized » Palladium-catalyzed direct C-H ethoxycarbonylation of 2-aryl-1,2,3-triazoles and efficient synthesis of ... Palladium-catalyzed direct C-H ethoxycarbonylation of 2-aryl-1,2,3-triazoles and efficient synthesis of suvorexant. ...
In this research, first project involves the synthesis and self-assembling properties of triazole containing glycoconjugates ... Design, Synthesis and Characterization of Triazole Based Glycoconjugates and 4,6-Acetal Protected D-Glucosamine Derivatives as ... In this research, first project involves the synthesis and self-assembling properties of triazole containing glycoconjugates ... "Design, Synthesis and Characterization of Triazole Based Glycoconjugates and 4,6-Acetal Protected D-Glucosamine Derivatives as ...
Antifungal effects of PC945, a novel inhaled triazole, on Candida albicans-infected immunocompromised mice. Yuki Nishimoto, ...
... the emergence of triazole-resistant A. fumigatus threatens the effectiveness of triazoles in clinical practice (3). Patients ... Patients can acquire triazole-resistant A. fumigatus infections because of exposure to long-term triazole therapy for chronic ... Fatal Fungicide-Associated Triazole-Resistant Aspergillus fumigatus Infection, Pennsylvania, USA On This Page ... Fatal Fungicide-Associated Triazole-Resistant Aspergillus fumigatus Infection, Pennsylvania, USA. Emerging Infectious Diseases ...
Cationic peptidomimetic amphiphiles having a n-aryl- or n-naphthyl-1,2,3-triazole core structure targeting clostridioides ( ... 3-triazole core structure targeting clostridioides (Clostridium) difficile: Synthesis, antibacterial evaluation and an in vivo ... 3-triazole core structure targeting clostridioides (Clostridium) difficile: Synthesis, antibacterial evaluation and an in vivo ...
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Triazoles exhibit biological activity, notably as antifungals, antimicrobials, and enzymatic inhibitors. BOC Sciences can ... provide varieties of triazole/tetrazole that are broadly applied in medicinal, organic, and material chemistry. ... Triazoles and tetrazoles are aromatic five-membered heterocycles containing respectively three and four nitrogen atoms. ... The formulas of Triazole and Tetrazole and tetrazole are C2H3N3 and CH2N4 respectively. (Fig.1). The isomeric 1,2,4-triazole ...
  • Of particular concern are resistant infections that appear to be related to environmental use of triazole fungicides in agriculture rather than to previous patient use of antifungal medicine. (cdc.gov)
  • Use of triazole fungicides in the environment increased more than fourfold from 2006 to 2016 in the United States, amplifying concerns about resistant A. fumigatus infections. (cdc.gov)
  • The agricultural use of triazole fungicides, a practice that recently increased 4-fold in the United States, can select for A. fumigatus strains harboring unique CYP51A gene mutations, such as TR 34 /L98H and TR 46 /Y121F/T289A, that can cause pan-triazole resistance in patients ( 5 , 6 ). (cdc.gov)
  • All TR 34 /L98H/S297T/F495I, TR 34 /L98H, and TR 46 /Y121F/T289A isolates exhibited cross-resistance to difenoconazole and tebuconazole (both triazole fungicides) without fitness cost, demonstrated by normal growth rates ( Appendix Figure 2). (cdc.gov)
  • A triazole antifungal agent that inhibits fungal cytochrome P450-mediated 14 alpha-lanosterol demethylation, which is essential in fungal ergosterol biosynthesis. (medscape.com)
  • Voriconazole (VRZ) is a second-generation triazole antifungal agent with broad-spectrum activity. (bvsalud.org)
  • We present here the synthesis and characterization of this triazole-based, self-immolative prochelator: TIP (4-(5-(2-((4-boronobenzyl)oxy)phenyl)-3-(2-hydroxyphenyl)-1H-1,2,4-triazol-1-yl)benzoic acid). (duke.edu)
  • Schiff bases, thiazole, and triazole derivatives are considered key scaffolds in medicinal chemistry. (chemaxon.com)
  • Synthesis and biological evaluation of a novel library of fused 1,2,3-triazole derivatives are described. (unc.edu.ar)
  • This article demonstrates the synthesis of 1,2,4-triazole derivatives and their applications in medicine particularly as anti-breast cancer agents which is a major issue of the present. (matheo.si)
  • We report a fatal infection in a 65-year-old immunocompromised male patient caused by pan-triazole-resistant Aspergillus fumigatus containing a TR 34 /L98H genetic mutation linked to agricultural fungicide use. (cdc.gov)
  • Average agricultural triazole fungicide use by year and compound type in metric tons, United States, 1992-2016. (cdc.gov)
  • Average agricultural triazole fungicide use by state over five time periods in metric tons, United States, 1992-2016. (cdc.gov)
  • Triazole fungicide use in California, 2017. (cdc.gov)
  • Disease reduction from the use of one or two sprays of a triazole fungicide (tebuconazole) was also simulated, based on previous meta-analytic estimates, and the response in yield was used in a profitability analysis. (elsevier.com)
  • Ribavirin is a synthetic guanosine analogue (1-beta-D-ribofuranosyl-1H-1,2,4-triazole-3-carboxamide) that inhibits viral replication by inhibiting DNA and RNA synthesis. (medscape.com)
  • A potent selective triazole aromatase inhibitor, which inhibits the biosynthesis of estrogen by inhibiting the aromatase enzyme C-450, which is a major factor in stimulating the growth of breast cancer cells. (raw-hormonepowders.com)
  • In this research, first project involves the synthesis and self-assembling properties of triazole containing glycoconjugates derived from peracetylated glucosides and galactosides, their characterization as well as their applications in metallogel formation, catalysis, sustained drug release and dye removal for waste-water treatment. (odu.edu)
  • Towards Water Soluble Mitochondria-Targeting Theranostic Osmium(II) Triazole-Based Complexes. (whiterose.ac.uk)
  • Taking advantage of the good stability of triazole-Au(I) complexes (TA-Au), we successfully achieved good reactivity of intermolecular hydroamination for both terminal and internal alkynes. (uga.edu)
  • They also function as simple lipophilic spacers displaying two substituents in the appropriate manner, where the connectivity patterns of the embedded tetrazole units bear a striking resemblance to those of their 1,2,3-triazole analogues. (bocsci.com)
  • We now have designed, synthesized, and evaluated eighteen new 1,2,3-triazole analogues for their SphK2 inhibitory activity using a ADP-Glo kinase assay, and explored their in vivo anti-tumor bioactivity. (wustl.edu)
  • A wide variety of aryl esters containing 1,2,3-triazoles were obtained in moderate to good yields. (newdrugapprovals.org)
  • Efficient palladium-catalyzed C-H ethoxycarbonylation of 2-aryl-1,2,3-triazoles was developed by using diethyl azodicarboxylate as the esterification reagent. (newdrugapprovals.org)
  • Voriconazole belongs to the triazole class of antifungal drugs and is a first-line treatment for invasive aspergillosis ( 1 ). (cdc.gov)
  • IMSEAR at SEARO: Pregnancy interceptive activity of triazoles, oxadiazoles & thiadiazoles. (who.int)
  • A new class of heterocycles pyrrolyl thiadiazoles, pyrrolyl oxadiazoles and pyrrolyl triazoles were prepared from arylsulfonylethenesulfonylacetic acid methyl ester and tested for their antimicrobial and cytotoxic activities. (iisc.ac.in)
  • Comparative Effectiveness of Echinocandins vs Triazoles or Amphotericin B Formulations as Initial Directed Therapy for Invasive Candidiasis in Children and Adolescents. (chop.edu)
  • We compared the effectiveness of echinocandins to triazoles or amphotericin B formulations (triazole/amphotericin B) as initial directed therapy for invasive candidiasis. (chop.edu)
  • Exposure groups were categorized by receipt of an echinocandin vs receipt of triazole/amphotericin B. Primary outcome was global response at 14 days following invasive candidiasis onset, adjudicated by a centralized data review committee. (chop.edu)
  • After exclusions, 541 participants (235 in the echinocandin group and 306 in the triazole/amphotericin B group) remained. (chop.edu)
  • Crude failure rates at 14 days for echinocandin and triazole/amphotericin B groups were 9.8% (95% confidence intervals [CI]: 6.0% to 13.6%) and 13.1% (95% CI: 9.3% to 16.8%), respectively. (chop.edu)
  • The adjusted 14-day risk difference between echinocandin and triazole/amphotericin B groups was -7.1% points (95% CI: -13.1% to -2.4%), favoring echinocandins. (chop.edu)
  • CDC has developed a plan to address the growing threat of triazole-resistant A. fumigatus and has begun the first phase of implementation. (cdc.gov)
  • Clinical and environmental surveillance of triazole-resistant A. fumigatus is needed in the United States to prevent spread and guide healthcare and agricultural practices. (cdc.gov)
  • however, the emergence of triazole-resistant A. fumigatus threatens the effectiveness of triazoles in clinical practice ( 3 ). (cdc.gov)
  • Patients can acquire triazole-resistant A. fumigatus infections because of exposure to long-term triazole therapy for chronic aspergillosis or by directly inhaling environmental spores that are already triazole-resistant ( 3 ). (cdc.gov)
  • We report a patient who died from an invasive infection caused by a pan-triazole-resistant A. fumigatus strain containing an environmentally acquired TR 34 /L98H mutation in CYP51A . (cdc.gov)
  • Fifteen thiazolyl-triazole Schiff bases were evaluated for their antibacterial activity, measuring the growth inhibition zone diameter, the minimum inhibitory concentration (MIC), and the minimum bactericidal concentration (MBC), against Gram-positive (Staphylococcus aureus, Listeria monocytogenes) and Gram-negative (Escherichia coli, Salmonella typhimurium, Pseudomonas aeruginosa) bacteria. (chemaxon.com)
  • The virtual screening concluded that thiazolyl-triazole Schiff base B8 is the best drug-like candidate, satisfying requirements for both safety and efficacy, being more potent against the bacterial gyrA than ciprofloxacin. (chemaxon.com)
  • The reactions of hafnium(IV) isopropoxide isopropanolate with 3-methyl-4-amino-S~triazol-5-thiol, 3-ethyl-4-amino-S-triazol-5-thiol and also with Schiff bases derived from amino triazoles with benzaldehyde, acetophenone, salicylaldehyde or o - hydroxyacetophenone have been carried out in different molar ratios l:n (n = 1 to 4) in refluxing benzene. (mssm.edu)
  • We report the first examples of GOAT inhibitors incorporating a triazole linkage as a biostable isosteric replacement for the ester bond in ghrelin and amide bonds in previously reported GOAT inhibitors. (fpwr.org)
  • These triazole-containing inhibitors exhibit sub-micromolar inhibition of the human isoform of GOAT (hGOAT), and provide a foundation for rapid future chemical diversification and optimization of hGOAT inhibitors. (fpwr.org)
  • The synthesized 1,2,4-triazole-naphthyl hybrids were screened for the anticancer activity against MCF-7 breast cancer lines. (matheo.si)
  • Antifungal triazole posaconazole targets an early stage of the parechovirus A3 life cycle. (cdc.gov)
  • The azide-alkyne Huisgen cycloaddition is a mild and selective reaction that gives 1,2,3-triazoles as products. (bocsci.com)
  • Fluconazole is in a class of antifungals called triazoles. (medlineplus.gov)
  • In the final step, benzylbromide undergoes SN 2 displacement with sodium triazole to give anastrozole. (gpatindia.com)
  • A chromatographic method for determination of 3-amino-5-mercapto-1,2,4-triazole in biological fluids. (cdc.gov)
  • Low, high, and average estimates of agricultural triazole use by year in metric tons, United States, 1992-2016. (cdc.gov)
  • We are seller of 1- [3- (Trifluoromethyl)benzyl]-1H-1,2,3-triazole-4-carbaldehyde. (hotelikdelfin.pl)
  • Pandey, OP 1988, ' Reactions of hafnium(iv) isopropoxide isopropanolate with mercapto triazoles ', Synthesis and Reactivity in Inorganic and Metal-Organic Chemistry , vol. 18, no. 6, pp. 575-591. (mssm.edu)
  • The inhibitive action of 3-amino-1,2,4-triazole (ATA) on 70Cu-30Zn alloy corrosion in HNO 3 0,5M was examined. (journaldephysique.org)
  • The corrosion mitigation behaviour of 1-benzyl-4-(naphthalen-2-yl)-1H-1,2,3-triazole (BNT) has been explored on mild steel in 1M HCl medium employing chemical and electrochemical techniques. (niscair.res.in)
  • Copper Corrosion Inhibition and Adsorption Behavior of 3-Amino-1,2,4-triazole [J]. Acta Phys. (pku.edu.cn)
  • Molecular modeling study was performed to elucidate the polar head group and 1,2,3-triazole pharmacophore impact on the SphK2 selectivity. (wustl.edu)
  • Triazoles and tetrazoles are aromatic five-membered heterocycles containing respectively three and four nitrogen atoms. (bocsci.com)
  • Treatment with triazoles, a class of antifungal medicine, has greatly improved survival, but resistant infections are increasingly reported worldwide. (cdc.gov)
  • People with a triazole-resistant infection have over a 30% higher likelihood of dying than patients with an infection that can be treated with these medicines. (cdc.gov)
  • 1-Sulfonyl-1,2,3-triazoles undergo a Doyle-Kirmse reaction upon treatment with allylic sulfides in the presence of a rhodium(II) catalyst to afford α-allyl-α-sulfanylimines. (elsevier.com)
  • Currently there are no citations for 3-[(1-Methyl-4-nitro-1H-imidazol-5-yl)thio]-4-methyl-1,2,4-triazole. (tocris.com)