Search results for "pyridines"
showing 10 items of 310 documents
Highly sensitive monoclonal antibody-based immunoassays for the analysis of fluopyram in food samples
2019
Monoclonal antibody-based techniques have become a useful analytical technology in the agro-food sector. Nowadays, residues of the recently registered fungicide fluopyram are increasingly being found in quality control programs. In the present study, novel chemical derivatives of this pesticide were prepared and specific and high-affinity monoclonal antibodies to fluopyram were raised for the first time. Moreover, immunoassays to fluopyram were developed in two alternative enzyme-linked immunosorbent assay formats, using homologous and heterologous assay conjugates, with limits of detection below 0.05 µg L−1. The optimized immunoassays were applied to the analysis of fluopyram in fortified …
Pyridylcarbene formation by thermal decomposition of 7-bromo-3-methyl-[1,2,3]triazolo[1,5-a]pyridine under pressure
2007
7-Bromo-3-methyl-[1,2,3]triazolo[1,5-a]pyridine 1 at 1.7 atm and 100ºC decompose to form a pyridylcarbene intermediate by nitrogen expulsion. The carbene stabilization give 2-bromo-6- vinylpyridine 2, 1-(6-bromopyridin-2-yl)ethanol 3, 1-(6-Bromopyridin-2-yl)ethanone 4, 2- bromo-6-[2-(6-bromopyridin-2-yl)-2-methyl-trans-cyclopropyl]pyridine 5, and 2-bromo-6-[2-(6- bromopyridin-2-yl)-2-methyl-cis-cyclopropyl]pyridine 6. Abarca Gonzalez, Belen, Belen.Abarca@uv.es ; Ballesteros Campos, Rafael, Rafael.Ballesteros@uv.es
Arylpyridines, arylpyrimidines and related compounds as potential modulator agents of the VEGF, hTERT and c-Myc oncogenes.
2019
Twenty-four derivatives structurally related to honokiol have been synthesized and biologically evaluated. IC50 values were determined towards the HT-29, MCF-7 and HEK-293 cell lines. Some of these derivatives exhibited comparable or lower IC50 values than honokiol towards the HT-29 and MCF-7 cell lines or else higher selectivity indexes than the natural product. Twelve selected derivatives were evaluated for their ability to inhibit the expression of the VEGFA, hTERT and c-Myc genes and also to inhibit the production of total c-Myc protein and the secretion of the VEGF protein. One of the most promising compounds, 3-(2,4-dimethoxyphenyl)pyridine, may be a good candidate for further studies…
Enzyme-responsive silica mesoporous supports capped with azopyridinium salts for controlled delivery applications
2012
11 páginas, 7 figuras, 3 tablas y 2 esquemas
Structural Determinants for the Mode of Action of Imidazopyridine DS2 at δ-Containing γ-Aminobutyric Acid Type A Receptors
2021
Despite the therapeutic relevance of δ-containing γ-aminobutyric acid type A receptors (GABAARs) and the need for δ-selective compounds, the structural determinants for the mode and molecular site of action of δ-selective positive allosteric modulator imidazo[1,2-a]pyridine DS2 remain elusive. To guide the quest for insight, we synthesized a series of DS2 analogues guided by a structural receptor model. Using a fluorescence-based fluorometric imaging plate reader membrane potential assay, we found that the δ-selectivity and the pharmacological profile are severely affected by substituents in the 5-position of the imidazopyridine core scaffold. Interestingly, the 5-methyl, 5-bromo, and 5-chl…
Hapten Synthesis and Polyclonal Antibody-Based Immunoassay Development for the Analysis of Forchlorfenuron in Kiwifruit
2010
High-affinity polyclonal antibodies directed against the synthetic cytokinin forchlorfenuron (CPPU) were produced from three immunizing haptens with equivalent spacer arms located at different positions. A competitive immunoassay was developed with a limit of detection in buffer of 12.42 +/- 3.06 ng/L. In addition, the ability of the produced antibodies to recognize a set of synthetic CPPU analogues was studied. It was evidenced that the linker position had a strong impact on the specificity of the generated polyclonals, which were more sensitive to changes at moieties of the target analyte located furthest from the derivatization site of the immunogen. Finally, matrix effects of gold and g…
Hapten synthesis, monoclonal antibody generation, and development of competitive immunoassays for the analysis of picoxystrobin in beer.
2010
Abstract This paper describes the original synthesis of a functionalized derivative of the fungicide picoxystrobin and the generation of the first reported monoclonal antibodies against this strobilurin pesticide. The synthetic hapten was prepared by total synthesis from commercial chemicals and incorporating the spacer arm through a carbon–carbon single bond. Also, to obtain the immunogen, an uncommon hapten activation strategy based on N,N′-disuccinimidyl carbonate was employed, affording high activation yields and clean and reproducible coupling results. With these immunoreagents, two enzyme-linked immunosorbent assays (ELISAs) were developed: a competitive one-step assay using the antib…
Kinetics of the lipoperoxyl radical-scavenging activity of indicaxanthin in solution and unilamellar liposomes
2007
Abstract The reaction of the phytochemical indicaxanthin with lipoperoxyl radicals generated in methyl linoleate methanol solution by 2,20-azobis(2,4-dimethylvaleronitrile), and in aqueous soybean phosphatidylcholine unilamellar liposomes by 2,20-azobis(2- amidinopropane)hydrochloride, was studied. The molecule acts as a chain-terminating lipoperoxyl radical scavenger in solution, with a calculated inhibition constant of 3.63 £ 105M21 s21, and a stoichiometric factor approaching 2. Indicaxanthin incorporated in liposomes prevented lipid oxidation, inducing clear-cut lag periods and decrease of the propagation rate. Both effects were concentration-dependent, but not linearly related to the p…
3-[4-(1H-indol-3-yl)-1,3-thiazol-2-yl]-1H-pyrrolo[2,3-b]pyridines, nortopsentin Analogues with antiproliferative activity
2015
A new series of nortopsentin analogues, in which the imidazole ring of the natural product was replaced by thiazole and the indole unit bound to position 2 of the thiazole ring was substituted by a 7-azaindole moiety, was efficiently synthesized. Two of the new nortopsentin analogues showed good antiproliferative effect against the totality of the NCI full panel of human tumor cell lines (~60) having GI50 values ranging from low micromolar to nanomolar level. The mechanism of the antiproliferative effect of these derivatives, investigated on human hepatoma HepG2 cells, was pro-apoptotic, being associated with externalization of plasma membrane phosphatidylserine and mitochondrial dysfunctio…
Antihyperalgesic and analgesic properties of the N-methyl-d-aspartate (NMDA) receptor antagonist neramexane in a human surrogate model of neurogenic …
2006
Abstract NMDA-receptors are a major target in the prevention and treatment of hyperalgesic pain states in neuropathic pain. However, previous studies revealed equivocal results depending on study design and efficacy parameters. We tested the analgesic (generalized reduction of generation and processing of nociceptive signalling) and anti-hyperalgesic (prevention of central sensitization) properties of the NMDA-receptor antagonist neramexane and the potassium channel opener flupirtine in the intradermal capsaicin injection model. Furthermore, we tested the effect on pain summation (wind up). Eighteen healthy subjects received either a single dose of neramexane (40 mg p.o.), flupirtine (100 m…