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991.
A synthesis of N-(8-Methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benz[b]azepin-3-yl)-benzamide 2 via an intramolecular amidoalkylation is described. 相似文献
992.
Francesca Gado Rebecca Ferrisi Sarah Di Somma Fabiana Napolitano Kawthar A. Mohamed Lesley A. Stevenson Simona Rapposelli Giuseppe Saccomanni Giuseppe Portella Roger G. Pertwee Robert B. Laprairie Anna Maria Malfitano Clementina Manera 《Molecules (Basel, Switzerland)》2022,27(9)
1,8-naphthyridine-3-carboxamide structures were previously identified as a promising scaffold from which to obtain CB2R agonists with anticancer and anti-inflammatory activity. This work describes the synthesis and functional characterization of new 1,8-naphthyridin-2(1H)-one-3-carboxamides with high affinity and selectivity for CB2R. The new compounds were able to pharmacologically modulate the cAMP response without modulating CB2R-dependent β-arrestin2 recruitment. These structures were also evaluated for their anti-cancer activity against SH-SY5Y and SK-N-BE cells. They were able to reduce the cell viability of both neuroblastoma cancer cell lines with micromolar potency (IC50 of FG158a = 11.8 μM and FG160a = 13.2 μM in SH-SY5Y cells) by a CB2R-mediated mechanism. Finally, in SH-SY5Y cells one of the newly synthesized compounds, FG158a, was able to modulate ERK1/2 expression by a CB2R-mediated effect, thus suggesting that this signaling pathway might be involved in its potential anti-cancer effect. 相似文献
993.
Iresha D. Herath Dr. Colum Breen Dr. Sarah H. Hewitt Dr. Thomas R. Berki Dr. Ahmad F. Kassir Dr. Charlotte Dodson Martyna Judd Dr. Shereen Jabar Dr. Nicholas Cox Prof. Gottfried Otting Dr. Stephen J. Butler 《Chemistry (Weinheim an der Bergstrasse, Germany)》2021,27(51):13009-13023
A lanthanide-binding tag site-specifically attached to a protein presents a tool to probe the protein by multiple spectroscopic techniques, including nuclear magnetic resonance, electron paramagnetic resonance and time-resolved luminescence spectroscopy. Here a new stable chiral LnIII tag, referred to as C12 , is presented for spontaneous and quantitative reaction with a cysteine residue to generate a stable thioether bond. The synthetic protocol of the tag is relatively straightforward, and the tag is stable for storage and shipping. It displays greatly enhanced reactivity towards selenocysteine, opening a route towards selective tagging of selenocysteine in proteins containing cysteine residues. Loaded with TbIII or TmIII ions, the C12 tag readily generates pseudocontact shifts (PCS) in protein NMR spectra. It produces a relatively rigid tether between lanthanide and protein, which is beneficial for interpretation of the PCSs by single magnetic susceptibility anisotropy tensors, and it is suitable for measuring distance distributions in double electron–electron resonance experiments. Upon reaction with cysteine or other thiol compounds, the TbIII complex exhibits a 100-fold enhancement in luminescence quantum yield, affording a highly sensitive turn-on luminescence probe for time-resolved FRET assays and enzyme reaction monitoring. 相似文献
994.
Robert Malmberg Dr. Tobias von Arx Monirul Hasan Dr. Olivier Blacque Atul Shukla Dr. Sarah K. M. McGregor Prof. Shih-Chun Lo Prof. Ebinazar B. Namdas Prof. Koushik Venkatesan 《Chemistry (Weinheim an der Bergstrasse, Germany)》2021,27(25):7265-7274
N-Heterocyclic carbene (NHC) cyclometalated gold(III) complexes remain very scarce and therefore their photophysical properties remain currently underexplored. Moreover, gold(III) complexes emitting in the blue region of the electromagnetic spectrum are rare. In this work, a series of four phosphorescent gold(III) complexes was investigated bearing four different NHC monocyclometalated (C^C*)-type ligands and a dianionic (N^N)-type ancillary ligand ((N^N)=5,5’-(propane-2,2-diyl)bis(3-(trifluoromethyl)-1 H-pyrazole) (mepzH2)). The complexes exhibit strong phosphorescence when doped in poly(methyl methacrylate) (PMMA) at room temperature, which were systematically tuned from sky-blue [λPL=456 nm, CIE coordinates: (0.20, 034)] to green [λPL=516 nm, CIE coordinates: (0.31, 0.54)] by varying the monocyclometalated (C^C*) ligand framework. The complexes revealed high quantum efficiencies (ϕPL) of up to 43 % and excited-state lifetimes (τ0) between 15–266 μs. The radiative rate constant values found for these complexes (kr=103–104 s−1) are the highest found in comparison to previously known best-performing monocyclometalated gold(III) complexes. Density functional theory (DFT) and time-dependent DFT (TD-DFT) calculations of these complexes further lend support to the excited-state nature of these complexes. The calculations showed a significant contribution of the gold(III) metal center in the lowest unoccupied molecular orbitals (LUMOs) of up to 18 %, which was found to be unique for this class of cyclometalated gold(III) complexes. Additionally, organic light-emitting diodes (OLEDs) were fabricated by using a solution process to provide the first insight into the electroluminescent (EL) properties of this new class of gold(III) complexes. 相似文献
995.
Dr. Jianlin Han Dr. Nataliya V. Lyutenko Dr. Alexander E. Sorochinsky Ayaka Okawara Dr. Hiroyuki Konno Dr. Sarah White Dr. Vadim A. Soloshonok 《Chemistry (Weinheim an der Bergstrasse, Germany)》2021,27(70):17510-17528
Over the recent years there has been a noticeable upsurge of interest in aza-analogs of tryptophan which are isosteric to the latter and found numerous applications in medicinal, bioorganic chemistry, and peptide research. In the present review article, five aza-tryptophan derivatives are profiled, including aza-substitution in the positions 2, on the five-membered ring, as well as in positions 4, 5, 6, and 7 on the six-membered ring. A detailed and comprehensive literature overview of the synthetic methods for the preparation of these aza-tryptophans is presented and general facets of the biological properties and most promising applications are discussed. 相似文献
996.
Many natural and artificial systems are subject to some sort of delay, which can be in the form of a single discrete delay or distributed over a range of times. Here, we discuss the impact of this distribution on (thermo-)dynamical properties of time-delayed stochastic systems. To this end, we study a simple classical model with white and colored noise, and focus on the class of Gamma-distributed delays which includes a variety of distinct delay distributions typical for feedback experiments and biological systems. A physical application is a colloid subject to time-delayed feedback control, which is, in principle, experimentally realizable by co-moving optical traps. We uncover several unexpected phenomena in regard to the system’s linear stability and its thermodynamic properties. First, increasing the mean delay time can destabilize or stabilize the process, depending on the distribution of the delay. Second, for all considered distributions, the heat dissipated by the controlled system (e.g., the colloidal particle) can become negative, which implies that the delay force extracts energy and entropy of the bath. As we show here, this refrigerating effect is particularly pronounced for exponential delay. For a specific non-reciprocal realization of a control device, we find that the entropic costs, measured by the total entropy production of the system plus controller, are the lowest for exponential delay. The exponential delay further yields the largest stable parameter regions. In this sense, exponential delay represents the most effective and robust type of delayed feedback. 相似文献
997.
Hassan H. Hammud Sarah A. Maache Nasreen Al Otaibi Nadeem S. Sheikh 《Molecules (Basel, Switzerland)》2022,27(21)
The corrosion inhibition effect of the three extracts from Harmal roots (HRE), leaves (HLE), and flowers (HFE) were studied for carbon steel corrosion inhibition in 0.25 M H2SO4 solution. The electrochemical impedance study indicated that the three types of extracts decreased corrosion effectively through a charge transfer mechanism. Harmal roots and leaf extracts showed inhibition values of 94.1% and 94.2%, while it was 88.7% for Harmal flower extract at the inhibitor concentration of 82.6 ppm. Potentiodynamic polarization data revealed that Harmal extracts acted through predominant cathodic type inhibition. Both the corrosion current density and corrosion rate decreased significantly in the presence of Harmal extracts compared to blank solution. The corrosion rate (mpy) value was 63.3, 86.1, and 180.7 for HRE, HLE, and HFE, respectively. The adsorption-free energy change ΔGads (kJ·mol−1) values calculated from the Langmuir adsorption isotherm plots were for HRE (−35.08), HLE (−33.17), and HFE (−33.12). Thus, corrosion inhibition occurred due to the adsorption of Harmal extract on the carbon steel surface via the chemisorption mechanism. Moreover, a computational investigation using B3LYP/6-311G++(d,p) basis set in both gaseous and aqueous phases was performed for the major alkaloids (1–8) present in the Harmal extract. 相似文献
998.
Ohne Zusammenfassung 相似文献
999.
1000.
Ohne Zusammenfassung 相似文献