Search results for "pyrimidine"
showing 10 items of 589 documents
Site-heterologous haptens and competitive monoclonal antibody-based immunoassays for pyrimethanil residue analysis in foodstuffs
2015
Pyrimethanil is a widely used post-harvest fungicide whose residues are commonly found in fruits and vegetables. We herein report the synthesis of two new functionalized derivatives of pyrimethanil carrying an equivalent spacer arm at different positions of the molecule. The influence of the linker tethering site on the affinity of monoclonal antibodies was shown. Moreover, the development of competitive immunoassays in different formats and with high sensitivity to the target analyte - IC50 values below 0.3μg/L - is described. Optimized assays were characterized by the determination of the limit of quantification, trueness, and precision using water-diluted QuEChERS extracts of fruits and …
Artificial increase of uracilemia during fluoropyrimidine treatment can lead to DPD deficiency misinterpretation
2021
Each year in France, >75 000 patients receive fluoropyrimidines, including 5-fluorouracil (5-FU) and its oral prodrug capecitabine (Xeloda), to treat digestive, breast and head and neck cancers.1 Among them, ∼20% will experience severe hematological and digestive toxicities and <2% will have a fatal outcome in the first two cycles. A part of these toxicities may result from a deficiency in dihydropyrimidine dehydrogenase (DPD) which catabolizes the endogenous uracil (U) into dihydrouracil (UH2) as well as 5-FU. In 2018, French Health Authorities [Haute Autorité de Santé (HAS) and Institut National du Cancer, (INCa)] recommended the evaluation of the enzymatic activity of DPD by measuring th…
2-(4-Toluidino)pyrimidine
1984
Aus der Kondensation von 4-Tolylguanidin (1) mil den β-Diketonen 2a-g gehen die 2-(4-Toluidino)pyrimidine 3a-g hervor, unter denen sich Vertreter mit antidiabetischer und antimykotischer Wirksamkeit befinden. Antidiabetic Agents, II: 2-(4-Toluidino)pyrimidines Condensations of 4-tolylguanidine (1) with the β-diketones 2a-g yield the 2-(4-toluidino)pyrimidines 3a-g which comprise compounds exhibiting antidiabetic and antimycotic activities.
Antimykotische wirkstoffe. XX . Fluorierte 2-(4-toluidino)pyrimidine
1985
Aus der Kondensation von 4-Tolylguanidin (1) mit den β-Diketonen 2a-f gehen die fluorierten 2-(4-Toluidino)pyrimidine 3a-f hervor. Strukturtyp 3 zeichnet sich durch antimykotische Wirkung aus. Condensation of 4-tolylguanidine (1) with the β-diketones 2a-f yields the fluorinated 2-(4-toluidino)pyrimidines 3a-f. Structures of type 3 exhibit antimycotic activity.
Antimykotische wirkstoffe. XIX. 4,6-Disubstituierte 2-(cyanamino)pyrimidine
1985
Aus der Umsetzung von Dicyandiamid (1) mit β-Diketonen (2a-c) gehen die 2-Cyanaminopyrimidine (3a-c) hervor. Strukturtyp 3 wird durch spektroskopische Daten gestutzt, wahrend gleichzeitig eine 1-Cyan-2-imino-struktur (4) ausgeschlossen wird. Verbindung 3a zeigt fungistatische und nematizide Wirkungen. The reaction of city dicyandiamide (1) with β-diketones 2a-c leads to 2-(cyanoamino)pyrimidines 3a-c. Structure type 3 is supported by spectroscopic data, while at the same time a 1-cyano-2-imino structure (4) is excluded. Compound 3a exhibits fungistatic and nematicidal activity.
The new 5- or 6-azapyrimidine and cyanuric acid derivatives of L-ascorbic acid bearing the free C-5 hydroxy or C-4 amino group at the ethylenic space…
2011
Abstract We report on the synthesis of the novel types of cytosine and 5-azacytosine (1–9), uracil and 6-azauracil (13–18) and cyanuric acid (19–22) derivatives of l -ascorbic acid, and on their cytostatic activity evaluation in human malignant tumour cell lines vs. their cytotoxic effects on human normal fibroblasts (WI38). The CD spectra analysis revealed that cytosine (5 and 6), uracil (14–16), 6-azauracil (17) and cyanuric acid (21) derivatives of l -ascorbic acid bearing free amino group at ethylenic spacer existed as a racemic mixture of enantiomers, whereas L-ascorbic derivatives containing the C-5 substituted hydroxy group at the ethylenic spacer were obtained in (4R, 5S) enantiomer…
Review of the safety, tolerability, and drug interactions of the new antifungal agents caspofungin and voriconazole
2003
Managing invasive fungal infections often presents a challenge for clinicians in the treatment of immunocompromised patients. Two very different systemic antifungal agents, voriconazole and caspofungin, have recently been introduced into the market place. Voriconazole is a new triazole antifungal, while caspofungin is the first echinocandin antifungal. Voriconazole acts by inhibiting the synthesis of ergosterol in the fungal cell membrane. Caspofungin inhibits beta-1,3-D-glucan synthesis in the cell wall, a target present in fungal cells, but absent from mammalian cells. Both agents are broad-spectrum, with efficacy against invasive Aspergillus and Candida infections. The safety and tolerab…
In vitro activity of fluconazole, voriconazole and caspofungin against clinical yeast isolates.
2007
Predicting the clinical outcome of a systemic mycosis is often a difficult task, especially when microbiological resistance is one of the factors contributing to therapeutic failure. Some of these factors are host-related--e.g. immune state, site and severity of infection, poor compliance to therapy--while others are associated with the drug's characteristics--e.g. dosage, type of compound (fungistatic/fungicidal), pharmacokinetic properties and drug-drug interactions. In the last few years, clinicians have been confronted with the problem of selecting the most appropriate antifungal therapy for systemic infections and have highlighted the need for a reliable method to assay the in vitro su…
Pharmacogenomics in colorectal carcinomas: Future perspectives in personalized therapy
2005
The recent introduction of new drugs such as capecitabine, irinotecan, and oxaliplatinum has greatly improved the clinical outcome of patients with advanced/metastatic colorectal cancer. Nevertheless, some patients may suffer from the adverse drug reactions which will probably be the main cause of chemotherapy failure. The goal of pharmacogenomics is to find correlations between therapeutic responses to drugs and the genetic profiles of patients; the different responses to a particular drug are due, in fact, not only to the specific clinico-pathological features of the patient or to environmental factors, but also to the ethnic origins and the particular individual's genetic profile. Genes …
Intracellular retention of ABL kinase inhibitors determines commitment to apoptosis in CML cells
2012
PLoS one 7(7), e40853 (2012). doi:10.1371/journal.pone.0040853