Search results for "stereo"
showing 10 items of 6147 documents
Identification of conjugation and cleavage products in the thiolytic metabolism of the anticancer drug 4'-(9-acridinylamino)methanesulfon-m-anisidide.
1981
Conjugation and cleavage products in the thiolytic metabolism of the anticancer drug 4′ -(9-acridinyl amino)methanesulfon-m-anisidide were identified primarily by high-pressure liquid chromatography in combination with field desorption mass spectrometry. The spontaneous metabolic pathway of the drug, as related to its susceptibility to nucleophilic attack by endogenous thiols at the 9-carbon atom of the acridine moiety, has been studied. Among the metabolite fraction of 4′-(9-acridinylamino)methanesulfon-m-anisidide excreted in rat bile after administration of a therapeutic dose, a conjugate was identified as the 9-acridinyl thioether of glutathione. This conjugation product and the corresp…
Synthesis and evaluation of 18F-fluoroethylated benzothiazole derivatives for in vivo imaging of amyloid plaques in Alzheimer's disease
2010
Amyloid aggregates play a major role in the development of Alzheimer's disease. Targeting these aggregates by PET probes enables non-invasively the detection and quantification of amyloid deposit distribution in human brains. Based on benzothiazole core structure a series of amyloid imaging agents were developed. Currently [(11)C]2-(4'-(methylamino)phenyl)-6-hydroxybenzothiazole (Pittsburgh Compound-B (PIB) is the most specific and widely used amyloid imaging ligand. But due to the short half life of (11)C, longer lived (18)F-labeled derivatives offer logistic advantages and higher contrast images. In this work, three different [(18)F]fluoroethoxy-substituted benzothiazole derivatives ([(18…
H2-Antihistaminika, 36. Mitt. Isolamtidin und Analoge
1987
Isolamtidin (9a), ein Stellungsisomer des Lamtidins (8a), sowie die analogen N3-substituierten 1-Methyl-1H-1,2,4-triazol-3,5-diamine 9e-i, k wurden durch spezifische Synthese dargestellt und am isolierten Meerschweinchenvorhof und an der histaminstimulierten Sauresekretion der narkotisierten Ratte auf H2-antagonistische Wirkung untersucht. H2-Antihistaminics, XXXVI: Isolamitidine and Analogues Isolamitidine (9a), a position isomer of lamtidine (8a), as well as the analogous N3-substituted 1-methyl-1H-1,2,4-triazole-3,5-diamines 9e-i, k were prepared and tested for H2-antagonistic activity on the isolated guinea-pig atrium and towards the histamine-stimulated acid secretion of the anaestheti…
Application of solid-phase microextraction combined with derivatization to the enantiomeric determination of amphetamines.
2005
Abstract The utility of combining chiral derivatization and solid-phase microextraction (SPME) for the enantiomeric analysis of primary amphetamines by liquid chromatography has been investigated. Different derivatization/extraction strategies have been evaluated and compared using the chiral reagent o -phthaldialdehyde (OPA)– N -acetyl- l -cysteine (NAC) and fibres with a Carbowax-templated resin coating. Amphetamine, norephedrine and 3,4-methylenedioxyamphetamine (MDA) were used as model compounds. On the basis of the results obtained, a new method is presented based on the derivatization of the analytes in solution followed by SPME of the OPA–NAC derivatives formed. The proposed conditio…
Off-line coupling of multidimensional immunoaffinity chromatography and ion mobility spectrometry: A promising partnership.
2015
The extreme specificity of immunoaffinity chromatography (IAC) columns coupled to the high sensitivity of ion mobility spectrometry (IMS) measurements makes this combination really useful for rapid, selective, and sensitive determination of a high variety of analytes in different samples. The capabilities of the IAC-IMS coupling have been highlighted under three different scenarios: (i) multiclass residue analysis using a single IAC column, (ii) multiclass residue analysis using stacked IAC columns, and (iii) isomer analysis. In the first case, the determination of three strobilurin fungicides - azoxystrobin, picoxystrobin, and pyraclostrobin - in water and strawberry juice was considered, …
Multivariate optimization approach for chiral resolution of drugs using human serum albumin in affinity electrokinetic chromatography-partial filling…
2005
The enantiomeric resolution of chiral compounds using HSA by means of affinity EKC (AEKC)-partial filling technique is the result of a delicate balance between different experimental variables such as protein concentration, running pH (background electrophoretic buffer, protein and compound solutions) and protein solution plug length. In this paper multivariate optimization approaches for chiral separation of four basic drugs (alprenolol, oxprenolol, promethazine and propranolol) using HSA as chiral selector in AEKC-partial filling technique are studied. The experimental conditions to achieve maximum resolution are optimized using the Box-Behnken experimental design. Partial least squares a…
Strategies for the enantiomeric determination of amphetamine and related compounds by liquid chromatography.
2002
This paper summarizes recent research on the stereospecific analysis of amphetamine, its analogs and metabolites, by liquid chromatography. The different methods proposed have been evaluated and compared in terms of resolution power, time of analysis, sensitivity, or potential for automation. Chiral derivatization, followed by separation of the diastereomers formed in achiral chromatographic systems, is still the method preferred for the analysis of amphetamines at trace levels, as derivatization also improves analyte detectability. This is the method of choice for the enantiomeric analysis of amphetamines at the low concentrations typically encountered in biological samples. In recent year…
Prediction of the chemiluminescent behavior of pharmaceuticals and pesticides.
2001
The present paper deals with the first attempt to apply molecular connectivity calculations to predict a chemical property with analytical usefulness: the chemiluminescent behavior of substances when reacted with common oxidants in a liquid phase. Preliminary evidence when searching for new direct CL methods consisted of the examination of analyte reaction with a wide range of oxidants and media. This task, which results in time-consuming and trial-and-error expensive procedures, is necessary due to ensure empirical or theoretical rules for CL prediction are available. On the other hand, in quantitative structure-activity relationship studies, molecular connectivity is a topological method …
Tips on ligand immobilization and kinetic study using surface plasmon resonance.
2016
Surface plasmon resonance (SPR) technique offers a robust label-free approach applicable in various investigations including binding affinity, specificity and kinetics of biological macromolecules (e.g., peptides, proteins and nucleotidase) and small molecules. SPR provides extremely important data on the kinetics and affinity of substances examined, through which bio-specific interaction(s) can be established by the analysis of adsorption of analyte onto the immobilized ligand(s) on a sensor-based analytical system. Due to SPR wide applications in biomedical laboratories, the aim of this editorial is to highlight the importance of SPR in affinity kinetics and ligand immobilization.
Reactions of platinum(iv)-bound nitriles with isomeric nitroanilines: addition vs. substitution
2012
The platinum(IV) complex trans-[PtCl(4)(EtCN)(2)] reacts smoothly and under mild conditions with isomeric o-, m- and p-nitroanilines (NAs) yielding two different types of products depending on the NA isomer, viz. the nitroaniline complexes cis/trans-[PtCl(4)(NA)(2)] (cis/trans-1-3) and the amidine species trans-[PtCl(4){NH=C(Et)NHC(6)H(4)NO(2)-m}(EtCN)] (4), trans-[PtCl(4){NH=C(Et)NHC(6)H(4)NO(2)-m}(2)] (5) and trans-[PtCl(4){NH=C(Et)NHC(6)H(4)NO(2)-p}(EtCN)] (6). Complexes 4 and 5 undergo cyclometalation, furnishing mer-[PtCl(3){NH=C(Et)NHC(6)H(3)NO(2)-m}(EtCN)] (7) and mer-[PtCl(3){NH=C(Et)NHC(6)H(4)NO(2)-m}{NH=C(Et)NHC(6)H(3)NO(2)-m}] (8), respectively. Moreover, 8 both in the solid stat…