Search results for "triazol"
showing 10 items of 598 documents
Erratum: Phase II study of sequential hormonal therapy with anastrozole/exemestane in advanced and metastatic breast cancer
2005
Hormonal therapy is the preferred systemic treatment for recurrent or metastatic, post-menopausal hormone-receptor-positive breast cancer. Previous studies have shown that there is no cross-resistance between exemestane and reversible aromatase inhibitors. Exposure to hormonal therapy does not hamper later response to chemotherapy. Patients with locally advanced or metastatic, hormonal receptor positive or unknown, breast cancer were treated with oral anastrozole, until disease progression, followed by oral exemestane until new evidence of disease progression. The primary end point of the study was clinical benefit, defined as the sum of complete responses (CR), partial responses (PR) and >…
A bis(triazole)benzamide receptor for the complexation of halide anions and neutral carboxylic acid guests. Guest-controlled topicity and self-assemb…
2012
Bis(triazole)benzamide 1 has been readily synthesized by means of Cu-catalyzed 1,3-dipolar cycloaddition and its ability to bind halide anions and neutral gallic acid derivative 12GA has been theoretically and experimentally investigated. The cavity defined by the N-H amide group and the vicinal aromatic hydrogens is suitable to form H-bonding arrays with halide guests. The stability of complexes 1·Cl- and 1·Br- is very similar, as DFT calculations predict and 1H NMR titration experiments confirm. The zigzag "anti" conformation of the molecule generates two regions with complementary positive and negative potentials that favor the statistical complexation of two molecules of the neutral car…
Peptides of the Constant Region of Antibodies Display Fungicidal Activity
2012
Synthetic peptides with sequences identical to fragments of the constant region of different classes (IgG, IgM, IgA) of antibodies (Fc-peptides) exerted a fungicidal activity in vitro against pathogenic yeasts, such as Candida albicans, Candida glabrata, Cryptococcus neoformans, and Malassezia furfur, including caspofungin and triazole resistant strains. Alanine-substituted derivatives of fungicidal Fc-peptides, tested to evaluate the critical role of each residue, displayed unaltered, increased or decreased candidacidal activity in vitro. An Fc-peptide, included in all human IgGs, displayed a therapeutic effect against experimental mucosal and systemic candidiasis in mouse models. It is in…
Antifungal drugs influence neutrophil effector functions
2019
There is a growing body of evidence for immunomodulatory side effects of antifungal agents on different immune cells, e.g., T cells. Therefore, the aim of our study was to clarify these interactions with regard to the effector functions of polymorphonuclear neutrophils (PMN). Human PMN were preincubated with fluconazole (FLC), voriconazole (VRC), posaconazole (POS), isavuconazole (ISA), caspofungin (CAS), micafungin (MFG), conventional amphotericin B (AMB), and liposomal amphotericin B (LAMB). PMN then were analyzed by flow cytometry for activation, degranulation, and phagocytosis and by dichlorofluorescein assay to detect reactive oxygen species (ROS). Additionally, interleukin-8 (IL-8) re…
Cellulose‑copper as bio-supported recyclable catalyst for the clickable azide-alkyne [3 + 2] cycloaddition reaction in water.
2018
Abstract Naturally-occurring cellulose has been employed as a bio-support macromolecule for the immobilization of either copper(I) or copper(II) ions in order to click azide and alkyne derivatives in water. Under such a click regime, 1,4-disubstitued-1,2,3-triazoles were obtained regioselectively in excellent yields at room temperature. The reaction work-up is simple and the bio-heterogeneous catalyst that has been fully characterized by AAS, SEM, EDX and FT-IR can be easily separated and reused at least five times without any significant decrease in its activity and selectivity, particularly in the case of the very stable CuI-Cellulose.
A combined experimental and theoretical study of the thermal cycloaddition of aryl azides with activated alkenes.
2011
International audience; Reactions were performed from aryl azides on the one hand, and activated alkenes coming from β-dicarbonyl compounds or malonodinitrile on the other hand, either with recourse to conventional heating or to microwave activation, to afford 1-aryl-1H-1,2,3-triazoles. The mechanism and the regioselectivity of the reactions involving β-dicarbonyl compounds have been theoretically studied using DFT methods at the B3LYP/6-31G* level: they are domino processes comprising a tautomeric equilibrium of the β-dicarbonyl compounds with their enol forms, a 1,3-dipolar cycloaddition of the enol forms with the aryl azides (high activation energy), and a dehydration process (lower acti…
Recent advances in copper-based solid heterogeneous catalysts for azide-alkyne cycloaddition reactions
2022
The copper(I)-catalyzed azide−alkyne cycloaddition (CuAAC) reaction is considered to be the most representative ligation process within the context of the “click chemistry” concept. This CuAAC reaction, which yields compounds containing a 1,2,3-triazole core, has become relevant in the construction of biologically complex systems, bioconjugation strategies, and supramolecular and material sciences. Although many CuAAC reactions are performed under homogenous conditions, heterogenous copper-based catalytic systems are gaining exponential interest, relying on the easy removal, recovery, and reusability of catalytically copper species. The present review covers the most recently developed copp…
Therapeutic tools for oral candidiasis : current and new antifungal drugs
2019
Background Candidiasis is one of the most common opportunistic oral infections that presents different acute and chronic clinical presentations with diverse diagnostic and therapeutic approaches. The present study carries out a bibliographic review on the therapeutic tools available against oral candidiasis and their usefulness in each clinical situation. Material and Methods Recent studies on treatment of oral candidiasis were retrieved from PubMed and Cochrane Library. Results Nystatin and miconazole are the most commonly used topical antifungal drugs. Both antifungal drugs are very effective but need a long time of use to eradicate the infection. The pharmacological presentations of mico…
Unique Bridging Function of the Triazole Core in Copper(II) Chloride Complexes with 1-Allylbenzotriazole
2005
During alternating-current electrochemical synthesis of copper(I) π-complex of [CuCl{C6H4N3(C3H5)}] composition, starting from ethanol solution, containing CuCl2·2H2O and 1-allylbenzotriazole, green crystals of intermediate [CuII3Cl6{C6H4N3(C3H5)}4] (I) compound has been obtained upon 24 h. After some days these crystals transform into red ones of [CuII2Cl4{C6H4N3(C3H5)}3] (II). Both compounds were X-Ray structurally investigated. Crystals of I are triclinic, sp.gr. a = 9.1329(9), b = 10.0352(4), c = 12.239(3) A, α = 76.443(13), β = 84.470(14), γ = 76.808(7)°, V = 1060.5(3) A3, R = 0.0414 for 3311 reflections. II: monoclinic, C2/c, a = 13.828(1), b = 15.044(2), c = 10.702(1) A, β = 91.36(1)…
Theoretical absorption and emission spectra of 1H- and 2H-benzotriazole
2003
Excitation energies, dipole moments, and transition properties for the lowest-lying 1(π, π*) and 1(n, π*) electronic states of two benzotriazole tautomers have been studied at the complete active space (CAS) SCF and multiconfigurational second-order perturbation (CASPT2) levels. With these results, the UV absorption spectra of 1H- and 2H-benzotriazole were first described individually, and then they were considered simultaneously in order to better understand the experimental, observed spectrum of benzotriazole. Aspects of the fluorescence of the compound have been also analyzed. The spectrum of benzotriazole is finally related to those of other azo-compounds.