Search results for "Mace"

A NEW DOPAMINE-AMINOACID CONJUGATE: SYNTHESIS AND DETERMINATION OF PHYSICO-CHEMICAL PROPERTIES USEFUL TO CROSS THE BBB

2012

Synthesis and biological activities of a new class of heat shock protein 90 inhibitors, designed by energy-based pharmacophore virtual screening

2013

The design through energy-based pharmacophore virtual screening has led to aminocyanopyridine derivatives as efficacious new inhibitors of Hsp90. The synthesized compounds showed a good affinity for the Hsp90 ATP binding site in the competitive binding assay. Moreover, they showed an excellent antiproliferative activity against a large number of human tumor cell lines. Further biological studies on the derivative with the higher EC50 confirmed its specific influence on the cellular pathways involving Hsp90.

Aminoquinolines: Fluorescent sensors to DNA – A minor groove probe. Experimental and in silico studies

2023

An aminoquinoline (AQ4) was developed and proven to be a new and efficient DNA minor groove fluorescent probe. The specificity for DNA minor groove was attested by comparing it with well-established DNA probes such as Hoechst stain, acridine orange, and ethidium bromide. AQ4 was similar to the Hoechst stain, a classic minor groove probe, and opposite to acridine orange and ethidium bromide, the typical intercalating probes. An advantage of AQ4 to the Hoechst stain was the higher fluorescent signal-to-noise ratio (+DNA/-DNA). The interaction with DNA leads to an exclusive fluorescent band centered at 590 nm. The red-shifted fluorescent band is associated with a new absorption band (490 nm), …

Imidazolsynthesen, 8. Mitt.: N-Substituierte Imidazole nach Weidenhagen

1976

Die Weidenhagen-Synthese N-unsubstituierter Imidazole aus α-substituierten Carbonylverbindungen 1, Aldehyden 3, wasrigem Ammoniak (4) und Kupfer(II)-salzen als Oxidationsmittel ist in Gegenwart primarer Amine 5 auch zur Darstellung N-substituierter Imidazole 6 geeignet. Weidenhagen Synthesis of N-Substituted Imidazoles The Weidenhagen synthesis of N-unsubstituted imidazoles from α-substituted carbonyl compounds 1, aldehydes 3, and aqueous ammonia (4) with copper (II) salts as oxidizing agents is also usable for the synthesis of N-substituted imidazoles 6 through the addition of primary amines 5.

Imidazolsynthesen, 10. Mitt. Zur selektiven Synthese N-substituierter Imidazol-4-äthanole

1977

Die Synthese N-substituierter Methoxyathylimidazole 5, 6 aus Aldehyden 1, 1-Hydroxy-4-methoxy-2-butanon (2), primaren Aminen 3 und Ammoniak (4) nach Weidenhagen liefert Gemische, in denen im GC die 1,4-Isomere 5 in der Regel deutlich uberwiegen. Aus diesen lassen sich durch Atherspaltung mit HJ die N-substituierten Imidazol-4-athanole 8 erhalten. Selective Synthesis of N-Substituted Imidazole-4-ethanols The synthesis of N-substituted methoxyethylimidazoles 5, 6 from aldehydes 1, 1-hydroxy-4-methoxy-2-butanone (2), primary amines 3, and ammonia (4), using the Weidenhagen cyclisation, yields mixtures in which, according to gc analysis, the 1,4-isomers 5 prevail. Ether cleavage with HI gives t…

Surfactant effect on the physicochemical characteristics of cationic solid lipid nanoparticles

2016

Solid lipid nanoparticles (SLNs) may be considered as a new approach for therapeutics for many diseases. In addition to drug delivery, their use as non-viral vectors for gene delivery can be obtained by including cationic lipids, which provide a positive surface potential that favors binding to the nucleic acids as DNA, siRNA, miRNA, etc. In fact, the addition of cationic surfactants is indispensable for obtaining nanoparticles with surface positive charge. In this study, three different cationic lipids (dioctadecyl dimethyl ammonium bromide, cetyltrimethyl ammonium bromide, cetylpyridinium chloride) and Brij 76 as nonionic surfactant were employed to formulate Precirol ATO 5 based cSLN usi…

Determination of barbiturates in urine by micellar liquid chromatography and direct injection of sample.

2000

Abstract A liquid chromatographic procedure for the determination of six barbiturates (barbital, diallyl barbituric acid, phenobarbital, butabarbital, amobarbital and pentobarbital) in urine samples is described. The proposed system uses a Spherisorb octadecyl-silane ODS-2 C 18 analytical column and a guard column of similar characteristics. The UV detector was set at 240 nm. A study to select adequate composition of the micellar mobile phase for the separation of these compounds in urine samples is performed. Maximum resolution was achieved with a 0.07 M sodium dodecylsulphate-0.3% propanol at pH 7.4 eluent. Limits of detection at 240 nm were ranged between 0.13 μg ml −1 for diallyl barbit…

Solapamiento del nicho trófico en un área de cría en la costa portuguesa

2002

The diets and the trophic niche overlap between seven flatfish species were studied in a coastal nursery adjoining to the Tagus estuary (Portugal). Fish were sampled monthly, from March to November 1999, using a beach seine. Arnoglossus imperialis (Rafinesque, 1810), Arnoglossus laterna (Walbaum, 1792) and Arnoglossus thori Kyle, 1913, fed mainly on crustaceans. The diets of Buglossidium luteum (Risso, 1810) and Dicologoglossa cuneata (Moreau, 1881) were mainly composed of Bivalvia and Polychaeta, while for Scophthalmus rhombus (Linnaeus, 1758) the main food items were Mysidacea and Teleostei. The diet of Pegusa lascaris (Risso, 1810) was mainly composed by Cumacea, Bivalvia, Decapoda and A…

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…