Search results for "pharmaceutical"

2020

Tristriazolotriazines (TTTs) with a threefold alkoxyphenyl substitution were prepared and studied by DSC, polarized optical microscopy (POM) and X-ray scattering. Six pentyloxy chains are sufficient to induce liquid-crystalline behavior in these star-shaped compounds. Thermotropic properties of TTTs with varying substitution patterns and a periphery of linear chains of different lengths, branching in the chain and swallow-tails, are compared. Generally, these disks display broad and stable thermotropic mesophases, with the tangential TTT being superior to the radial isomer. The structure–property relationships of the number of alkyl chains, their position, length and structure were studied.

Inulin vinyl sulfone derivative cross-linked with bis-amino PEG: new materials for biomedical applications

2009

In this work new hydrogels based on biocompatible polymers such as inulin (INU) and O,O'-bis(2-aminoethyl)polyethyleneglycol (PEGBa) have been prepared and charaterized. In particular, INU has been derivatized with divinyl sulfone (DV) thus obtaining the INUDV derivative, a copolymer bearing double bonds highly reactive towards the conjugate addition by nucleophilic molecules. INUDV has been characterized by FT-IR, 1 H-NMR and SEC analyses that have confirmed the success of the derivatization reaction. With the aim to obtain novel hydrogel systems, INUDV derivative has been cross-linked with PEGBa in phosphate buffer solution pH 7.4. The reaction has been carried out for 4 h at room tempera…

Multicomponent solid dispersion a new generation of solid dispersion produced by spray-drying

2020

Abstract The term “multicomponent solid dispersion” is widely used in recent literature to describe solid formulations consisting of a special excipient's mixture and active molecules finely dispersed. However, this term has not yet been defined. In this review, we aimed to improve the definition of multicomponent solid dispersions as a new generation of solid dispersions capable to improve both formulation issues and the therapeutic effect of the final dosage form. As it is well-known the use of solid dispersions to improve drug dissolution rate and solubility, this review describes the field of solid dispersions as well as the formulation strategies available for their production. In part…

The Quest for Mononuclear Gold(II) and Its Potential Role in Photocatalysis and Drug Action.

2017

The chemistry of gold strongly focuses on the ubiquitous oxidation states +I and +III. The intermediate oxidation state +II is generally avoided in mononuclear gold species. In recent years, gold(II) has been increasingly suggested as a key intermediate in artificial photosynthesis systems, with gold(III) moieties acting as electron acceptors, as well as in gold-catalyzed photoredox catalysis and radical chemistry. This Minireview provides a concise summary of confirmed and characterized mononuclear open-shell gold(II) complexes. Recent findings on structural motifs and reactivity patterns will be discussed. Exciting developments in the fields of photosynthesis, photocatalysis, and potentia…

Molecular topology: a useful tool for the search of new antibacterials.

2000

Molecular topology has been applied to find new lead antibacterial compounds. Among the selected compounds, hesperidin, neohesperidin and Mordant Brown 24 stand out, with minimum inhibitory concentrations 90, MIC90<0.3 mg / mL.

Zur C-17-Oxidation von Clavinalkaloiden mit primärer alkoholischer Hydroxylgruppe

1975

Die Oppenauer-Oxidation von 1 mit Cyclohexanon fuhrt zu dem Aldolkondensationsprodukt 4 und der Carbonsaure 3. Analog konnte Lysergsaure (8) in geringer Menge aus 6 gewonnen und im Reaktionsgemisch von 7 nachgewiesen werden. Damit wurden erstmals Clavinalkaloide mit primarer alkoholischer Hydroxylgruppe chemisch zu den entsprechenden Carbonsauren oxidiert. C-17-Oxidation of Clavine Alkaloids with a Primary Alcoholic Hydroxyl Group. 1 is converted by Oppenauer oxidation with cyclohexanone to the aldol condensation product 4 and to the carboxylic acid 3. Lysergic acid (8) was obtained in a small yield by the analogous reaction of 6 and was found in the reaction mixture of 7. Thus clavine alka…

2020

The facile synthesis and detailed investigation of a class of highly potent protease inhibitors based on 1,4-naphthoquinones with a dipeptidic recognition motif (HN-l-Phe-l-Leu-OR) in the 2-position and an electron-withdrawing group (EWG) in the 3-position is presented. One of the compound representatives, namely the acid with EWG = CN and with R = H proved to be a highly potent rhodesain inhibitor with nanomolar affinity. The respective benzyl ester (R = Bn) was found to be hydrolyzed by the target enzyme itself yielding the free acid. Detailed kinetic and mass spectrometry studies revealed a reversible covalent binding mode. Theoretical calculations with different density functionals (DFT…

Radiolabeling of DOTATOC with the long-lived positron emitter 44Sc.

2010

Abstract The positron-emitting radionuclide 44 Sc with a half-life of 3.97 h and a β + branching of 94.3% is of potential interest for clinical PET. As so far it is available from a 44 Ti/ 44 Sc generator in Mainz, where long-lived 44 Ti decays to no-carrier-added (nca) 44 Sc. The 44 Sc is a trivalent metal cation and should be suitable for complexation with many well established bifunctional chelators conjugated to peptides or other molecular targeting vectors. Thus, the aim of this work was to investigate the potential of 44 Sc for labeling of DOTA-conjugated peptides. DOTA-D-Phe 1 -Tyr 3 -octreotide (DOTATOC) was used as a model molecule to study and optimize labeling procedure. Reaction…

Molecular hydrogen (H 2 ) as a potential treatment for acute and chronic fatigue

2020

Many diseases as well as acute conditions can lead to fatigue, which can be either temporary or chronic in nature. Acute fatigue develops frequently after physical exercise or after alcohol hangover, whereas microbial infections such as influenza or COVID-19 and chronic diseases like Parkinson's disease or multiple sclerosis are often associated with chronic fatigue. Oxidative stress and a resulting disturbance of mitochondrial function are likely to be common denominators for many forms of fatigue, and antioxidant treatments have been shown to be effective in alleviating the symptoms of fatigue. In this study, we review the role of reactive oxygen and nitrogen species in fatigue and the an…

Enhanced Skin Permeation of Estradiol by Dimethyl Sulfoxide Containing Transdermal Patches.

2021

Dimethyl sulfoxide is a well-known and widely used dermal penetration enhancer. Its incorporation in transdermal patches would be highly desirable