Search results for "substitution"

First case in Italy of acquired resistance to oseltamivir in an immunocompromised patient with influenza A/H1N1v infection

2010

A pandemic influenza A/H1N1v strain with the neuraminidase H274Y mutation was detected in nasal secretions of a 2-year-old leukemic patient with influenza-like illness after 18 days of treatment with oseltamivir. At baseline, no drug-resistant virus was found, while 4 days after treatment initiation a mix- ture of wild-type and mutated virus was detected. After treatment interruption, the wild type influenza virus re-emerged and became prevalent in nasal secretions after a few days, suggesting the lower fitness of the mutated virus strain. The patient slowly improved concurrently with a decrease in virus load, which resulted negative 42 days after diagnosis. No other drug-resistant influenz…

Inter- and Intramolecular Anodic Nucleophilic Substitutions of Porphyrins. Reactivity of the resulting products

2020

This manuscript presents the functionalization of porphyrins by anodic nucleophilic substitution (SNAn). After an introduction describing generalities on porphyrin, the 2nd chapter deals with the 2-step synthesis of primary aminoporphyrins. The 1st electrochemical step consists in oxidizing the porphyrin at the 1st oxidation potential in the presence of pyridine. The formed pyridinium-porphyrin is then transformed into an amine by opening the pyridinium fragment by nucleophilic attack of piperidine.The 3rd chapter presents the synthesis and redox reactivity of porphyrins substituted with one (or several) aromatic groups carrying an imine function (thiopyrimidine, quinoline and aminopyridine…

Functional characterisation of alpha-galactosidase a mutations as a basis for a new classification system in fabry disease.

2013

Fabry disease (FD) is an X-linked hereditary defect of glycosphingolipid storage caused by mutations in the gene encoding the lysosomal hydrolase α-galactosidase A (GLA, α-gal A). To date, over 400 mutations causing amino acid substitutions have been described. Most of these mutations are related to the classical Fabry phenotype. Generally in lysosomal storage disorders a reliable genotype/phenotype correlation is difficult to achieve, especially in FD with its X-linked mode of inheritance. In order to predict the metabolic consequence of a given mutation, we combined in vitro enzyme activity with in vivo biomarker data. Furthermore, we used the pharmacological chaperone (PC) 1-deoxygalacto…

Reactions of electron-rich heterocycles with orthocarboxylic acid derivatives.11. Reactions of carbazole and 4-methoxycarbazole with triethyl orthofo…

1988

Carbazole (1a) and 4-methoxycarbazole (1b) can be regioselectively functionalized by reaction with triethyl orthoformate. Whereas the reaction of 1a with the ortho ester furnishes the amide acetal 2, the new carbazole derivatives 4–10 are formed, depending on the reaction conditions, in the electrophilic substitution of 1b. The products of this reaction sequence provide a contribution to studies on the mechanism of the transformation of 1b to tris-carbazolylmethane 5. Compound 5 represents a new, three-bladed propeller in the triheteroarylmethane series.

Heterodimer formation of wild-type and amyotrophic lateral sclerosis-causing mutant Cu/Zn-superoxide dismutase induces toxicity independent of protei…

2008

Recent studies provide evidence that wild-type Cu/Zn-superoxide dismutase (SOD1(hWT)) might be an important factor in mutant SOD1-mediated amyotrophic lateral sclerosis (ALS). In order to investigate its functional role in the pathogenesis of ALS, we designed fusion proteins of two SOD1 monomers linked by a polypeptide. We demonstrated that wild-type-like mutants, but not SOD1(G85R) homodimers, as well as mutant heterodimers including SOD1(G85R)-SOD1(hWT) display dismutase activity. Mutant homodimers showed an increased aggregation compared with the corresponding heterodimers in cell cultures and transgenic Caenorhabditis elegans, although SOD1(G85R) heterodimers are more toxic in functiona…

Synthesis, biological evaluation, and: In silico studies of novel chalcone: In pyrazoline-based 1,3,5-triazines as potential anticancer agents

2020

A novel series of triazin-chalcones (7,8)a-g and triazin-N-(3,5-dichlorophenyl)pyrazolines (9,10)a-g were synthesized and evaluated for their anticancer activity against nine different cancer strains. Triazine ketones 5 and 6 were synthesized from the cyanuric chloride 1 by using stepwise nucleophilic substitution of the chlorine atom. These ketones were subsequently subjected to a Claisen-Schmidt condensation reaction with aromatic aldehydes affording chalcones (7,8)a-g. Then, N-(3,5-dichlorophenyl)pyrazolines (9,10)a-g were obtained by cyclocondensation reactions of the respective chalcones (7,8)a-g with 3,5-dichlorophenylhydrazine. Among all the evaluated compounds, chalcones 7d,g and 8g…

13C NMR study on the methoxy carbon chemical shifts in chloro-substituted anisoles and guaiacols

1983

The 13C NMR chemical shifts of methoxy carbons in chlorinated anisoles and guaiacols have been measured for acetone-d6 solutions. Multiple linear regression analysis, and also ‘simple sum rule’ calculations, have been used to estimate the effects of the chlorine atoms (the position and degree of substitution) on the chemical shifts. The most important effects have shown to be due to the chlorine atoms adjacent to the methoxy and hydroxy substituents. For chlorinated guaiacols, the greatest effect is due to the chlorine atom adjacent to the methoxy group. For chlorinated anisoles, the substituents adjacent to the methoxy group (2,6-disubstitution) cause large effects. For both groups of comp…

Zur Konstitutionsaufklärung trisubstituierter Indolderivate: NMR-spektroskopische Untersuchung von Bis(2,3-dimethyl-6-indolyl)-arylmethanen

1987

The application of combined1H- and13C-NMR-technics is used exemplarily for the elucidation of the type of substitution at the phenyl nucleus of indoles in 6,6′-bis-indolylarylmethanes (1,2). These methods can be applied in general to analogous structure problems.

Electrophilic Aromatic Substitution. VonR. Taylor. Wiley, Chichester 1990. XVI, 513 S., geb. £ 85.00 — ISBN 0-471-92482-2

1991

Syntheses and characterization of novel ruthenium complexes based on 1,3-dicyanobenzene

2007

Submitted by António Freitas (amsf@uma.pt) on 2019-06-14T13:25:52Z No. of bitstreams: 1 Syntheses and Characterization of Novel Ruthenium Complexes Based on 13-DicyanobenzeneJoãoRodrigues.pdf: 354444 bytes, checksum: edc8aaaa84900d75321648e76e0c8e27 (MD5) Made available in DSpace on 2019-06-14T13:25:52Z (GMT). No. of bitstreams: 1 Syntheses and Characterization of Novel Ruthenium Complexes Based on 13-DicyanobenzeneJoãoRodrigues.pdf: 354444 bytes, checksum: edc8aaaa84900d75321648e76e0c8e27 (MD5) Previous issue date: 2007 info:eu-repo/semantics/publishedVersion