23 research outputs found
Supplementary data for the article: PenjiÅ”eviÄ, J. Z.; Å ukaloviÄ, V. V.; AndriÄ, D. B.; RogliÄ, G. M.; NovakoviÄ, I. T.; Å oÅ”kiÄ, V.; KostiÄ-RajaÄiÄ, S. V. Synthesis, Biological Evaluation and Docking Analysis of Substituted Piperidines and (2-Methoxyphenyl)Piperazines. Journal of the Serbian Chemical Society 2016, 81 (4), 347ā356. https://doi.org/10.2298/JSC151021097P
Supplementary material for: [https://doi.org/10.2298/JSC151021097P]Related to published version: [http://cherry.chem.bg.ac.rs/handle/123456789/1937
Investigation of Antibacterial Activity of Cinnamyl Derivatives of Arylpiperazine
The derivatives of cinnamic acid and N-arylpiperazine show antibacterial activity. In this work the potential synergistic effect of cinnamyl derivatives of arylpiperazine in selected bacteria was investigated. The antibacterial activities of the derivatives were evaluated against Gram-positive bacteria: Staphylococcus aureus, Streptosporangium longisporum, Sarcina lutea, Micrococcus flavus, Clostridium sporogenes and Bacillus subtilis and Gram-negative bacteria: Escherichia coli, Pseudomonas aeruginosa, Salmonella enteritidis and Proteus vulgaris by the disc diffusion method. The minimum inhibitory concentration (MIC) against the selected bacteria was determined for all compounds that showed activity in the disc diffusion method. The majority of the investigated compounds displayed in vitro antibacterial activity. The effect of the type and structure of the substituent on the aromatic ring on the antibacterial activity is discussed. It was found that two derivatives expressed activity toward S. longisporum and P. aeruginosa that was almost as strong as that of amikacin
Supplementary data for article : KolareviÄ, S.; MilovanoviÄ, D.; KraÄun-KolareviÄ, M.; KostiÄ, J.; Sunjog, K.; MartinoviÄ, R.; ÄorÄeviÄ, J.; NovakoviÄ, I.; SladiÄ, D.; VukoviÄ-GaÄiÄ, B. Evaluation of Genotoxic Potential of Avarol, Avarone, and Its Methoxy and Methylamino Derivatives in Prokaryotic and Eukaryotic Test Models. Drug and Chemical Toxicology 2019, 42 (2), 130ā139. https://doi.org/10.1080/01480545.2017.1413108
Supplementary material for: [https://doi.org/10.1080/01480545.2017.1413108]Related to published version: [http://cherry.chem.bg.ac.rs/handle/123456789/322
Synthesis, biological evaluation and docking analysis of substituted piperidines and (2-methoxyphenyl)piperazines
A series of sixteen novel substituted piperidines and (2-methoxyphenyl)piperazines were synthesized, starting from the key intermediates 1-(2-methoxyphenyl)-4-(piperidin-4-yl)piperazine and 1-(2-methoxyphenyl)-4-[(piperidin-4-yl)methyl] piperazine. Biological evaluation of the synthesized compounds was illustrated by seven compounds, of which 1-(2-methoxyphenyl)-4-{[1-(2-nitrobenzyl) piperidin-4-yl] methyl} piperazine had the highest affinity for the dopamine D-2 receptor. For all seven selected compounds, docking analysis was performed in order to establish their structure-to-activity relationship.Supplementary material: [http://cherry.chem.bg.ac.rs/handle/123456789/3630
Supplementary data for the article: PenjiÅ”eviÄ, J. Z.; Å ukaloviÄ, V. V.; AndriÄ, D. B.; RogliÄ, G. M.; NovakoviÄ, I. T.; Å oÅ”kiÄ, V.; KostiÄ-RajaÄiÄ, S. V. Synthesis, Biological Evaluation and Docking Analysis of Substituted Piperidines and (2-Methoxyphenyl)Piperazines. Journal of the Serbian Chemical Society 2016, 81 (4), 347ā356. https://doi.org/10.2298/JSC151021097P
Supplementary material for: [https://doi.org/10.2298/JSC151021097P]Related to published version: [http://cherry.chem.bg.ac.rs/handle/123456789/1937
Synthesis and pharmacological evaluation of N-{4-[2-(4-arylpiperazin-1-yl) ethyl] phenyl}arylamides
Serotonin 5HT1a receptor belongs to a class of G-protein coupled receptors. It serves as a
potential target for neurological disorders such as depression, anxiety etc. It is a well-known
fact that N-arylpiperazine moiety is present in compounds with pronounced 5HT1a activity.
Taking into account previously published results1
novel structures of N-{4-[2-(4-
arylpiperazin-1-yl)ethyl]phenyl}arylamides (Figure 1.) were designed for target synthesis.
Proposed modifications include: different position of hydroxyl group in aryl amide part of
molecule and addition of methoxy and chloro substituents to the phenyl ring of parent
compounds, since their introduction in the molecule leads to increased receptor affinity.
New compounds were synthesized by acylation of N-arylpiperazines using 4-
nitrophenylacetic acid. Obtained amides were converted in 1-(4-nitrophenethyl)-4-
arylpiperazines using diborane in THF. Reduction of nitro compounds by Ra/Ni provided 1-
(4-aminophenethyl)-4-arylpiperazines. Target arylamides were obtained by condensation 1-
(4-aminophenethyl)-4-arylpiperazines with corresponding aryl acids in presence of
propylphosphoric acid anhydride (PPAA) in DMF.
All newly synthesized compounds were evaluated for their activity toward 5HT1a receptors
by in vitro competitive displacement assay of [3H] 8-OH-DPAT. HEK cell line were used as a
source of 5HT1a receptors.
Introduction of 2-methoxy and 2,3-dichloro groups,as well as meta and para hydroxyl group
in molecule resulted in increment of affinity toward 5HT1a receptors comparing to the parent
compounds
Supplementary data for article : KolareviÄ, S.; MilovanoviÄ, D.; KraÄun-KolareviÄ, M.; KostiÄ, J.; Sunjog, K.; MartinoviÄ, R.; ÄorÄeviÄ, J.; NovakoviÄ, I.; SladiÄ, D.; VukoviÄ-GaÄiÄ, B. Evaluation of Genotoxic Potential of Avarol, Avarone, and Its Methoxy and Methylamino Derivatives in Prokaryotic and Eukaryotic Test Models. Drug and Chemical Toxicology 2019, 42 (2), 130ā139. https://doi.org/10.1080/01480545.2017.1413108
Supplementary material for: [https://doi.org/10.1080/01480545.2017.1413108]Related to published version: [http://cherry.chem.bg.ac.rs/handle/123456789/322
Development of fluorinated indanone-based derivatives for the imaging of monoamine oxidase B via positron emission tomography
Ziel/Aim The monoamine oxidase B (MAO B) isoenzyme is known to be
involved in the oxidative deamination of biogenic amines. While the use of
MAO B inhibitors is already well-established for the treatment of Parkinsonās
disease, recent reports suggest its involvement in certain types of brain
tumors.1 We herein aim at the synthesis and preclinical evaluation of fluorinated indanone-based derivatives targeting MAO B in the brain via positron
emission tomography (PET).
Methodik/Methods A small series of fluorinated indanone derivatives
was obtained via the O-alkylation or esterification starting with the
commercially available 6-hydroxy-2,3-dihydro-1H-inden-1-one in one or
two steps. Binding affinities towards the human MAO isoenzymes were
estimated in vitro by radioligand displacement. HL126 was selected for
radiofluorination via its corresponding boronic acid pinacol ester. In
vitro autoradiography of [18F]HL126 was performed in mice brain slices.
In vivo evaluation of [18F]HL126 in CD-1 mice was carried out and
metabolism studies were performed in plasma and brain samples via
radio-HPLC.
Ergebnisse/Results The fluorinated indanone derivatives were synthesized
in yields ranging from 65-89 %. The fluorophenyl ether derivative, HL126,
was further selected for radiofluorination based on its high binding affinity
towards MAO B (Ki = 6.9 Ā± 5.3 nM). [18F]HL126 was obtained by an alcohol-enhanced copper-mediated approach via the corresponding boronic
acid pinacol ester precursor with radiochemical yields of about 11 Ā± 3 %,
high radiochemical purities (ā„99 %) and molar activities in the range of 20
GBq/mmol. In vitro autoradiography showed a specific blockade with
selective MAO-A/B inhibitors. PET/MRI analyses revealed that [18F]HL126
readily enters the brain. Some radiometabolites do cross the blood-brain
barrier.
Schlussfolgerungen/Conclusions Although metabolism studies with [18F]
HL126 revealed the presence of radiometabolites in the brain, the high binding affinity towards MAO B and the pronounced selectivity in in vitro autoradiography studies encourage further derivatization of indanone-based
scaffolds for targeting MAO B
Review of research, development and application of photovoltaic/thermal water systems
Among the many techniques for obtaining heat and electricity, solar thermal collectors, photovoltaic (PV) technology and PV/thermal (PV/T) technology have a very important place. The PV/T collectors enable the simultaneous conversion of solar radiation into thermal and electrical energy in a single device, with better space utilization and cost efficiency during construction. Specially designed PV/T collectors can replace the outer walls or roof covers and can be widely used in private houses, flat complexes, hospitals, schools, tourist and other objects for water heating and electrical energy generation. Due to their great application potential, hybrid collectors have been the subject of very intensive scientific research and technical development for many years. In this review article, the focus is on the research, development and application of the PV/T water systems in the last 10 years. The main task of researchers and manufacturers is to increase the efficiency of PV modules and thermal absorbers, using new materials and design types as well as their proper integration into the PV/T collector. It is also necessary to reduce the cost of these systems and make them more competitive in the market. In addition, the importance of PV/T systems is in providing energy in clean and environmentally friendly ways
Silicon increases phosphorus (P) uptake by wheat under low P acid soil conditions
Although silicon (Si) is known to improve plant growth under low phosphorus (P) conditions, the in planta mechanisms responsible for this effect are still unknown. Here, we investigated the role of Si on P uptake along with the expression of Pi transporters in wheat (Triticum aestivum L.) grown in low P acid soil in comparison with P fertilization and liming. A combined approach was performed including analyses of rhizosphere soil, tissue P content, the expression of the root Pi transporter genes (TaPHT1.1 and TaPHT1.2), and the root exudation of citrate and malate. Supply of Si in a form of Na2SiO3 increased shoot P concentration to an adequate level in the range of P-fertilized plants. Silicon ameliorated low soil pH and high Al3+ comparable to the effect of liming. The in planta effect of Si on up-regulating the expression of TaPHT1.1 and TaPHT1.2 was several fold higher and consequently P uptake doubled compared to both P fertilization and liming. In addition, Si directly stimulated root Pi acquisition by prominently increasing both malate and citrate exudation rate. Application of Si increased root exudation of organic acids that mobilize Pi in the rhizosphere and up-regulated Pi transporters in wheat roots