Search results for "DISCOVERY"
showing 10 items of 4119 documents
Äther und Ester des 4-(2-Hydroxyaethyl)-imidazols und Ester der 4-Imidazolpropionsäure 4. Mitt. über Struktur-Wirkungs-Beziehungen bei Histaminanaloga
1974
Als potentiell histaminartig wirksame Substanzen wurden Ather und Ester des 4-(2-Hydroxyaethyl)-imidazols und Ester der 4-Imidazolpropionsaure dargestellt und am isolierten Ileum des Meerschweinchens und anderen Testobjekten untersucht. Ethers and Esters of 4-(2-Hydroxyethyl)-imidazole and Esters of 4-Imidazolepropionic Acid As substances with possible histamine-like activity, ethers and esters of 4-(hydroxyethyl)-imidazole and esters of 4-imidazolepropionic acid are prepared and tested on isolated guinea pig ileum and other objects.
Ester des 4-Hydroxymethyl-imidazols und der 4-Imidazolessigsäure 2. Mitt. über Struktur-Wirkungs-Beziehungen bei Histaminanaloga
1974
Als potentiell histaminartig wirksame Substanzen wurden Ester des 4-Hydroxymethyl-imidazols und der 4-Imidazolessigsaure dargestellt und am isolierten Ileum des Meerschweinchens und anderen Testobjekten untersucht. Esters of 4-Hydroxymethylimidazole and 4-Imidazoleacetic Acid As substances with possible histamine-like activity esters of 4-hydroxymethylimidazole and 4-imidazoleacetic acid were prepared and tested on isolated guinea-pig ileum and other objects.
Direct radiofluorination of [18F]MH.MZ for 5-HT2A receptor molecular imaging with PET
2012
Imaging the serotonin 2A neuroreceptor with positron emission tomography has been carried out with [11C]MDL 100907 and [18F]altanserin for years. Recently, the MDL 100907 analogue [18F]MH.MZ was developed by combining the increased selectivity profile of MDL 100907 and the favourable radiophysical properties of fluorine-18. Here, we want to report the synthesis of [18F]MH.MZ via direct radiofluorination. Unfortunately, the direct radiofluorination did not have any significant benefits over the indirect labelling method. This is mainly because the precursor for the direct labelling approach is not completely stable and slowly decomposes. However, only one HPLC separation is necessary for the…
Organochromium complexes - labelled aminoglycoside antibiotics derived from kanamycin A and tobramycin. Synthesis, structural characterization and us…
1993
Abstract The synthesis of metallocenic derivatives of aminoglycoside antibiotics, i. e. kanamycin A and tobramycin, is described. The organometallic-labelled compounds have been obtained from the reaction between the polyaminodrugs and organochromium esters of N-hydroxysuccinimide. The reaction proceeded selectively at the 6′-N position, as might be deduced both from the mass and the pH-dependent 13 C-NMR spectra. The procedure could be regarded as generally useful for the metallolabelling of aminoglycoside antibiotics. As an example of application a competitive immunoassay based on the use of these labels is proposed.
Tropane-derived11C-labelled and18F-labelled DAT ligands
2013
Radiolabelling of cocaine-derived 3-phenyltropanes for dopamine transporter positron emission tomography with 18F and 11C is reviewed. Copyright © 2013 John Wiley & Sons, Ltd.
Targeting Orthosteric and Allosteric Pockets of Aromatase via Dual-Mode Novel Azole Inhibitors
2020
[Image: see text] Breast cancer (BC) is the most diffused cancer type in women and the second leading cause of death among the female population. Effective strategies to fight estrogen responsive (ER+) BC, which represents 70% of all BC cases, rely on estrogen deprivation, via the inhibition of the aromatase enzyme, or the modulation of its cognate estrogen receptor. Current clinical therapies significantly increased patient survival time. Nevertheless, the onset of resistance in metastatic BC patients undergoing prolonged treatments is becoming a current clinical challenge, urgently demanding to devise innovative strategies. In this context, here we designed, synthesized, and performed in …
Anti-inflammatory agents from plants: Progress and potential
2011
The identification of substances that can promote the resolution of inflammation in a way that is homeostatic, modulatory, efficient, and well-tolerated by the body is of fundamental importance. Traditional medicines have long provided front-line pharmacotherapy for many millions of people worldwide. Medicinal extracts are a rich source of therapeutic leads for the pharmaceutical industry. The use of medicinal plant therapies to treat chronic illness, including rheumatoid arthritis (RA) and inflammatory bowel disease (IBD), is thus widespread and on the rise.The aim of this review is to present recent progress in clinical anti-inflammatory studies of plant extracts and compound leads such a…
Investigations on the Steroidal Anti-Inflammatory Activity of Triterpenoids fromDiospyros leucomelas*
1995
Three triterpenes were isolated from Diospyros leucomelas and identified as betulin, betulinic acid, and ursolic acid. They showed anti-inflammatory activity in the carrageenan and serotonin paw edema tests and TPA and EPP ear edema tests. The blockade of their effects by progesterone, actinomycin D, and cycloheximide has served to determine the mechanism of action in relationship with that of glucocorticoids. Betulinic acid was the most affected and therefore a mode of action similar to these drugs may be postulated for it.
Essential Oil Composition of Alluaudia procera and in Vitro Biological Activity on Two Drug-Resistant Models
2019
Drug resistance is a major obstacle in antibiotic and antitumor chemotherapy. In response to the necessity to find new therapeutic strategies, plant secondary metabolites including essential oils (EOs) may represent one of the best sources. EOs in plants act as constitutive defenses against biotic and abiotic stress, and they play an important role in the pharmacology for their low toxicity, good pharmacokinetic and multitarget activity. In this context, natural products such as EOs are one of the most important sources of drugs used in pharmaceutical therapeutics. The aim of this paper was to identify the chemical composition of the essential oil of Alluaudia procera leaves, obtained by hy…
Quinoline anticancer agents active on DNA and DNA-interacting proteins: From classical to emerging therapeutic targets.
2021
Quinoline is one of the most important and versatile nitrogen heterocycles embodied in several biologically active molecules. Within the numerous quinolines developed as antiproliferative agents, this review is focused on compounds interfering with DNA structure or with proteins/enzymes involved in the regulation of double helix functional processes. In this light, a special focus is given to the quinoline compounds, acting with classical/well-known mechanisms of action (DNA intercalators or Topoisomerase inhibitors). In particular, the quinoline drugs amsacrine and camptothecin (CPT) have been studied as key lead compounds for the development of new agents with improved PK and tolerability…