Search results for "Perazine"
showing 10 items of 240 documents
5-HT3 receptor-channels coupled with Na+ influx in human T cells: role in T cell activation.
1999
The study was conducted on a human (Jurkat) T cell line, loaded with a Na+ fluorescent probe, SBFI/AM. Serotonin and an agonist of 5-HT3 receptor-channels, 2-methyl-5HT, evoked Na+ influx, whereas the agonists of other serotonergic receptor subtypes, i.e., 5-HT1A and 5-HT1B receptors, failed to induce Na+ influx in these cells. By using 3H-BRL43694, an agonist of 5-HT3 receptor-channels, we characterized 5-HT3 lymphocyte receptors which exhibited a density (Bmax) of 300 +/- 20 fmol/10(6) cells and a Kd of 30 nM in Jurkat T cells. The T-cell 5-HT3 receptor-channel is not regulated either by the protein kinase C or by the free intracellular calcium concentrations as the agents known to activa…
Solution processable piperazine and triphenyl moiety containing non-symmetric bis-styryl-DWK type molecular glasses with light-emitting and amplified…
2018
A series of 2,6-bis-styryl-4H-pyran-4-ylidene fragment containing glassy organic compounds with chemically stable bonding of amorphous phase promoting bulky triphenyl moieties through piperazine structural fragment (DWK-T dyes) in a form of 2-(5,5,5-triphenylpentyl)piperazin-1-yl)styryl)-substituent have been synthesized and investigated as the potential gain medium component for organic solid state laser applications. Physical properties of the dyes vary and are mostly depending from the other styryl-substituent attached to the 4H-pyran-4-ylidene backbone fragment in 6-position. Thermal stability of synthesized dyes is above 312°C with the glass transitions from 97°C to 109°C. Obtained nea…
From attraction to repulsion : anion–π interactions between bromide and fluorinated phenyl groups
2011
Anion–π interactions in crystals of fluorobenzyl ammonium salts depend on the degree of fluorination at the aromatics.
Biomimetic diels–alder cyclizations for the construction of the brevianamide, paraherquamide, sclerotamide, asperparaline and VM55599 ring systems
1998
Abstract A potentially bio-mimetic Diels–Alder cyclization to construct the bicyclo[2.2.2] ring system common to the paraherquamides, marcfortines, sclerotamides, brevianamides, VM55599, and asperparaline is reported. Epi-deoxybrevianamide E (22) is converted into the corresponding lactim ether (23) and then oxidized with DDQ to provide an azadiene (24) which is tautomerized in the presence of base to azadiene 25 which, spontaneously cyclizes to give a 2:1 mixture of cycloadducts 26 and 27. These cycloadducts are each in turn, converted into d , l -C-19-epi-brevianamide A (20) and d , l -brevianamide B (6). The stereochemical implications of the [4+2] cycloaddition is discussed in the conte…
Synthesis and Influence of 3-Amino Benzoxaboroles Structure on Their Activity against Candida albicans
2020
Benzoxaboroles emerged recently as molecules of high medicinal potential with Kerydin®
Mechanochemical synthesis of antifungal bis(benzoxaboroles)
2020
Several piperazine bis(benzoxaboroles) have been obtained both in solution as well as in the solid state. The environmentally friendly mechanochemical approach – hitherto not applied for the preparation of benzoxaboroles – was particularly beneficial in the case of two products afforded in low yields in solution. The in vitro studies showed high potential of the studied bis(fluorobenzoxaboroles) as antifungal agents, highlighting also the influence of the fluorine substituent position on their microbiological activity. The highest activity against A. niger, A. terreus, P. ochrochloron, C. tenuis and C. albicans was displayed by the analogue of the known benzoxaborole antifungal drug Kerydin…
Synthesis and structural elucidation of novel antifungal N-(fluorophenyl)piperazinyl benzoxaboroles and their analogues
2019
Abstract Series of novel N-(fluorophenyl)piperazine derivatives of phenylboronic compounds including benzoxaboroles, phenylboronic acids and phenylboronic methyl monoester have been obtained by facile synthetic methods starting from 2-formylphenylboronic acid. Molecular and crystal structures of those novel derivatives have been investigated by single crystal X-ray diffraction method. The Bond Valence Vector Model was used to describe strains in the boron coordination sphere. Microbiological activity of novel benzoxaboroles as well as their corresponding acid analogues against: A. niger, A. terreus, P. ochrochloron, C. tenuis and F. dimerum has been evaluated. The presence of heterocyclic b…
CO2 capture from biogas: Absorbent selection
2013
The development of proper biogas upgrading technology offers a viable means to utilize biogas in conventional power systems. In this paper, various molecular and ionic solvent systems were evaluated for CO2 removal from biogas in a loop reactor system. The performance of amine solutions, ionic liquids and their mixtures, amino acid salts and solutions blended with piperazine was compared in terms of their CO2 loading capacity. The experimental results revealed that addition of small amounts of piperazine can increase on average by 30 vol% the efficiency of above-mentioned solutions. The CO2 capturing capacity achieved for the most promising solvents was in the range of 50–60 L CO2/L absorbe…
Autoinhibition of nicotinic release of noradrenaline from postganglionic sympathetic nerves
1970
1. The effects of nicotine, DMPP (1,1-dimethylphenylpiperazine) and acetylcholine (plus atropine) on the isolated rabbit heart were investigated. Heart rate, amplitude of contraction, coronary flow and output of noradrenaline into the perfusate were recorded. Noradrenaline was estimated fluorimetrically. 2. All nicotinic drugs evoked a dose-dependent output of noradrenaline and increased the rate and the amplitude of contraction. Increases of heart rate in response to nicotine and DMPP and increases of amplitude of contraction in response to all nicotinic drugs were clearly related to the output of noradrenaline. 3. The dose-response curves of the noradrenaline output evoked by nicotine, DM…
A muscarinic inhibition of the noradrenaline release evoked by postganglionic sympathetic nerve stimulation
1969
1. The noradrenaline output from isolated rabbit hearts perfused with Tyrode solution was estimated fluorimetrically. The postganglionic sympathetic nerves of the heart were stimulated (10 shocks/sec; 1 msec) for three 1 min periods with intervals of 10 min. 2. The noradrenaline output evoked by 3 consecutive stimulation periods decreased exponentially. 3. Acetylcholine (10−9–10−6 g/ml) administered continuously one min before to one min after the second stimulation caused a dose-dependent reduction of the noradrenaline output evoked by the second stimulation to as low as 19% of the normal value. Acetylcholine in the concentrations applied did not cause a noradrenaline output by itself. 4. …