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61.
Karen Rodríguez-Villar Lilin Ypez-Mulia Miguel Corts-Gines Jacobo David Aguilera-Perdomo Edgar A. Quintana-Salazar Kevin Samael Olascoaga Del Angel Francisco Corts-Benítez Juan Francisco Palacios-Espinosa Olivia Soria-Arteche Jaime Prez-Villanueva 《Molecules (Basel, Switzerland)》2021,26(8)
Indazole is an important scaffold in medicinal chemistry. At present, the progress on synthetic methodologies has allowed the preparation of several new indazole derivatives with interesting pharmacological properties. Particularly, the antiprotozoal activity of indazole derivatives have been recently reported. Herein, a series of 22 indazole derivatives was synthesized and studied as antiprotozoals. The 2-phenyl-2H-indazole scaffold was accessed by a one-pot procedure, which includes a combination of ultrasound synthesis under neat conditions as well as Cadogan’s cyclization. Moreover, some compounds were derivatized to have an appropriate set to provide structure-activity relationships (SAR) information. Whereas the antiprotozoal activity of six of these compounds against E. histolytica, G. intestinalis, and T. vaginalis had been previously reported, the activity of the additional 16 compounds was evaluated against these same protozoa. The biological assays revealed structural features that favor the antiprotozoal activity against the three protozoans tested, e.g., electron withdrawing groups at the 2-phenyl ring. It is important to mention that the indazole derivatives possess strong antiprotozoal activity and are also characterized by a continuous SAR. 相似文献
62.
63.
Benjamin C. Ponedel Edgar Knobloch 《The European physical journal. Special topics》2016,225(13-14):2549-2561
We study spatial localization in the real subcritical Ginzburg-Landau equation u t = m 0 u + Q(x)u + u xx + d|u|2 u ?|u|4 u with spatially periodic forcing Q(x). When d>0 and Q ≡ 0 this equation exhibits bistability between the trivial state u = 0 and a homogeneous nontrivial state u = u 0 with stationary localized structures which accumulate at the Maxwell point m 0 = ?3d 2/16. When spatial forcing is included its wavelength is imprinted on u 0 creating conditions favorable to front pinning and hence spatial localization. We use numerical continuation to show that under appropriate conditions such forcing generates a sequence of localized states organized within a snakes-and-ladders structure centered on the Maxwell point, and refer to this phenomenon as forced snaking. We determine the stability properties of these states and show that longer lengthscale forcing leads to stationary trains consisting of a finite number of strongly localized, weakly interacting pulses exhibiting foliated snaking. 相似文献
64.
Dr. Andrew T. Krueger Dr. Carsten Kroll Edgar Sanchez Prof. Linda G. Griffith Prof. Barbara Imperiali 《Angewandte Chemie (International ed. in English)》2014,53(10):2662-2666
Described is the development and application of a versatile semisynthetic strategy, based on a combination of sortase‐mediated coupling and tetrazine ligation chemistry, which can be exploited for the efficient incorporation of tunable functionality into chimeric recombinant proteins. To demonstrate the scope of the method, the assembly of a set of bivalent ligands, which integrate members of the epidermal growth factor (EGF) ligand family, is described. By using a series of bivalent EGFs with variable intraligand spacing, the differences in structure were correlated with the ability to bias signaling in the ErbB receptor family in a cell motility assay. Biasing away from EGFR‐HER2 dimerization with a bivalent EGF was observed to reduce cell motility in an intraligand distance‐dependent fashion, thus demonstrating the utility of the approach for acutely perturbing receptor‐mediated cell signaling pathways. 相似文献
65.
Edgar Uhl Peter Mayer Henry Dube 《Angewandte Chemie (International ed. in English)》2020,59(14):5730-5737
Light‐driven molecular motors possess immense potential as central driving units for future nanotechnology. Integration into larger molecular setups and transduction of their mechanical motions represents the current frontier of research. Herein we report on an integrated molecular machine setup allowing the transmission of potential energy from a motor unit onto a remote receiving entity. The setup consists of a motor unit connected covalently to a distant and sterically encumbered biaryl receiver. By action of the motor unit, single‐bond rotation of the receiver is strongly accelerated and forced to proceed unidirectionally. The transmitted potential energy is directly measured as the extent to which energy degeneration is lifted in the thermal atropisomerization of this biaryl. Energy degeneracy is reduced by more than 1.5 kcal mol?1, and rate accelerations of several orders of magnitude in terms of the rate constants are achieved. 相似文献
66.
Diego Alberto Lomelí-Rosales Adalberto Zamudio-Ojeda Oscar Kevin Reyes-Maldonado Morelia Eunice Lpez-Reyes Georgina Cristina Basulto-Padilla Edgar Jos Lopez-Naranjo Víctor Manuel Zuiga-Mayo Gilberto Velzquez-Jurez 《Molecules (Basel, Switzerland)》2022,27(5)
So far, several studies have focused on the synthesis of metallic nanoparticles making use of extracts from the fruit of the plants from the genus Capsicum. However, as the fruit is the edible, and highly commercial, part of the plant, in this work we focused on the leaves, a part of the plant that is considered agro-industrial waste. The biological synthesis of gold (AuNPs) and silver (AgNPs) nanoparticles using aqueous extracts of root, stem and leaf of Capsicum chinense was evaluated, obtaining the best results with the leaf extract. Gold and silver nanoparticles synthesized using leaf extract (AuNPs-leaf and AgNPs-leaf, respectively) were characterized by UV-visible spectrophotometry (UV-Vis), Fourier Transform Infrared Spectroscopy with Attenuated Total Reflection (FTIR-ATR), X-ray Photoelectron Spectroscopy (XPS), Ultra Hight Resolution Scanning Electron Microscopy coupled to Energy-Dispersive X-ray spectroscopy (UHR-SEM-EDX) and Transmission Electron Microscopy (TEM), and tested for their antioxidant and antimicrobial activities. In addition, different metabolites involved in the synthesis of nanoparticles were analyzed. We found that by the use of extracts derived from the leaf, we could generate stable and easy to synthesize AuNPs and AgNPs. The AuNPs-leaf were synthesized using microwave radiation, while the AgNPs-leaf were synthesized using UV light radiation. The antioxidant activity of the extract, determined by ABTS, showed a decrease of 44.7% and 60.7% after the synthesis of the AuNPs-leaf and AgNPs-leaf, respectively. After the AgNPs-leaf synthesis, the concentration of polyphenols, reducing sugars and amino acids decreased by 15.4%, 38.7% and 46.8% in the leaf extract, respectively, while after the AuNPs-leaf synthesis only reducing sugars decreased by 67.7%. These results suggest that these groups of molecules are implicated in the reduction/stabilization of the nanoparticles. Although the contribution of these compounds in the synthesis of the AuNPs-leaf and the AgNPs-leaf was different. Finally, the AgNPs-leaf inhibited the growth of S. aureus, E. coli, S. marcescens and E. faecalis. All of them are bacterial strains of clinical importance due to their fast antibiotic resistance development. 相似文献
67.
68.
Edgar Baumeister Heinz Oberhammer Heinar Schmidt Ralf Steudel 《Heteroatom Chemistry》1991,2(6):633-641
The vapor phase structure of (CH3O)2S [1] has been investigated by electron diffraction and ab initio MO calculations, which both result in a C2 symmetry for the most stable geometry, the Cs conformer being less stable by about 12 kJ/mol. The torsional barrier for rotation about one SO bond was calculated as 37 kJ/mol (trans barrier). The geometrical parameters (electron diffraction) of the C2 conformer are: dSO = 162.5(2), dCO = 142.6(3), dCH = 110.5(7) pm angles OSO = 103(1)°, SOC = 115.9(4)°, HCH = 109(1)°, torsional angle COSO = 84(3)°. Geometrical data calculated with 6-31G* basis set agree well with the diffraction data; calculated dipole moments 1.1 D (C2) and 3.3 D (Cs). The infrared spectrum of gaseous (CH3O)2S and the Raman spectra of liquid and solid (CH3O)2S are reported and have been almost fully assigned to the 27 fundamental vibrations. 相似文献
69.
70.
Thane H. Taylor Nicholas W. Frost Michael T. Bowser Edgar A. Arriaga 《Analytical and bioanalytical chemistry》2014,406(6):1683-1691
Mitochondria are responsible for maintaining a variety of cellular functions. One such function is the interaction and subsequent import of proteins into these organelles via the translocase of outer membrane (TOM) complex. Antibodies have been used to analyze the presence and function of proteins comprising this complex, but have not been used to investigate variations in the abundance of TOM complex in mitochondria. Here, we report on the feasibility of using capillary cytometry with laser-induced fluorescence to detect mitochondria labeled with antibodies targeting the TOM complex and to estimate the number of antibodies that bind to these organelles. Mitochondria were fluorescently labeled with DsRed2, while antibodies targeting the TOM22 protein, one of nine proteins comprising the TOM complex, were conjugated to the Atto-488 fluorophore. At typical labeling conditions, 94 % of DsRed2 mitochondria were also immunofluorescently labeled with Atto-488 Anti-TOM22 antibodies. The calculated median number of Atto-488 Anti-TOM22 antibodies bound to the surface of mitochondria was ~2,000 per mitochondrion. The combination of fluorescent immunolabeling and capillary cytometry could be further developed to include multicolor labeling experiments, which enable monitoring several molecular targets at the same time in the same or different organelle types. Figure
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