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61.
To understand the substitution effects of 3-aminomethyl-pyridine on the reaction equilibrium, the interactions between a series of 3-aminomethyl-pyridine derivatives and peroxovanadium(V) complex [OV(O2)2(D2O)]?/[OV(O2)2(HOD)]? in solution were explored by the combined use of multinuclear (1H, 13C, and 51V) magnetic resonance spectroscopy together with HSQC in 0.15 M NaCl ionic medium for mimicking the physiological conditions. Some direct NMR data are given for the first time. The relative reactivity among the 3-aminomethyl-pyridine derivative ligands are N-(pyridin-3-ylmethyl)acetamide (1) ≈ N-(pyridin-3-ylmethyl)propionamide (2) > N-(pyridin-3-ylmethyl)pivalamide (3) > t-butyl(pyridin-3-ylmethyl)carbamate (4). The competitive coordination results in the formation of a series of new six-coordinate peroxovanadium species [OV(O2)2L]? (L = 1–4). The results of density functional calculations indicated that the solvation effects play an important role in these reactions, providing a reasonable explanation on the relative reactivity of the 3-aminomethyl-pyridine derivatives. 相似文献
62.
Shang Wu Hongheng Yu Qinzheng Hu Quanlu Yang Shouwang Xu Tian Liu 《Tetrahedron letters》2017,58(51):4763-4765
A silver-catalyzed decarboxylative cross-coupling of α-keto acids with alkenes is reported. The method, with a wide range of substrate tolerance and mild operational conditions, can produce various chalcone derivatives in moderate to high yields from easily available starting materials. 相似文献
63.
《Mathematische Nachrichten》2017,290(10):1544-1552
Let K and S be locally compact Hausdorff spaces and X be an abstract space. Suppose that T is a positive Banach lattice isomorphism from into . Then for each ordinal α the cardinalities of the αth derivatives and satisfy the following inequality Moreover, if then is a continuous image of a subset of which can be taken closed when K is compact. The first statement of this result for is a vector‐valued extension of a Cengiz's theorem and the second one is vector‐valued version of a Holsztyński's theorem. A simple example shows that the number is sharp in these vector‐valued theorems. 相似文献
64.
Hassan Khosravian‐Arab Mehdi Dehghan M. R. Eslahchi 《Mathematical Methods in the Applied Sciences》2017,40(18):6389-6410
This paper presents 2 new classes of the Bessel functions on a compact domain [0,T] as generalized‐tempered Bessel functions of the first‐ and second‐kind which are denoted by GTBFs‐1 and GTBFs‐2. Two special cases corresponding to the GTBFs‐1 and GTBFs‐2 are considered. We first prove that these functions are as the solutions of 2 linear differential operators and then show that these operators are self‐adjoint on suitable domains. Some interesting properties of these sets of functions such as orthogonality, completeness, fractional derivatives and integrals, recursive relations, asymptotic formulas, and so on are proved in detail. Finally, these functions are performed to approximate some functions and also to solve 3 practical differential equations of fractionalorders. 相似文献
65.
Yan Zhou Jinjian Li Han Yuan Rui Su Yue Huang Yiyou Huang Zhe Li Yinuo Wu Haibin Luo Chen Zhang Ling Huang 《Molecules (Basel, Switzerland)》2021,26(10)
Phosphodiesterase 2 (PDE2) has been regarded as a novel target for the treatment of Alzheimer’s disease (AD). In this study, we obtained (R)-LZ77 as a hit compound with moderate PDE2 inhibitory activity (IC50 = 261.3 nM) using a high-throughput virtual screening method based on molecular dynamics. Then, we designed and synthesized 28 dihydropyranopyrazole derivatives as PDE2 inhibitors. Among them, compound (+)-11h was the most potent PDE2 inhibitor, with an IC50 value of 41.5 nM. The molecular docking of PDE2-(+)-11h reveals that the 4-(trifluoromethyl)benzyl)oxyl side chain of the compound enters the H-pocket and forms strong hydrophobic interactions with L770/L809/F862, which improves inhibitory activity. The above results may provide insight for further structural optimization of highly potent PDE2 inhibitors and may lay the foundation for their use in the treatment of AD. 相似文献
66.
Huijuan Yang Yuyu Zhang Fang Zhou Juanjuan Guo Jiajie Tang Yanqing Han Zhanming Li Caili Fu 《Molecules (Basel, Switzerland)》2021,26(1)
Chitosan, a biopolymer possessing numerous interesting bioactivities and excellent technological properties, has received great attention from scientists in different fields including the food industry, pharmacy, medicine, and environmental fields. A series of recent studies have reported exciting results about improvement of the properties of chitosan using the Maillard reaction. However, there is a lack of a systemic review about the preparation, bioactivities and applications in food industry of chitosan-based Maillard reaction products (CMRPs). The presence of free amino groups in chitosan allows it to acquire some stronger or new functional properties via the Maillard reaction. The present review aims to focus on the current research status of synthesis, optimization and structural identification of CMRPs. The applications of CMRPs in the food industry are also discussed according to their biological and technological properties such as antioxidant, antimicrobial activities and inducing conformational changes of allergens in food. Some promising directions for future research are proposed in this review, aiming to provide theoretical guidance for the further development of chitosan and its derivatives. 相似文献
67.
Anna Carbone Stella Cascioferro Barbara Parrino Daniela Carbone Camilla Pecoraro Domenico Schillaci Maria Grazia Cusimano Girolamo Cirrincione Patrizia Diana 《Molecules (Basel, Switzerland)》2021,26(1)
Anti-virulence strategy is currently considered a promising approach to overcome the global threat of the antibiotic resistance. Among different bacterial virulence factors, the biofilm formation is recognized as one of the most relevant. Considering the high and growing percentage of multi-drug resistant infections that are biofilm-mediated, new therapeutic agents capable of counteracting the formation of biofilms are urgently required. In this scenario, a new series of 18 thiazole derivatives was efficiently synthesized and evaluated for its ability to inhibit biofilm formation against the Gram-positive bacterial reference strains Staphylococcus aureus ATCC 25923 and S. aureus ATCC 6538 and the Gram-negative strain Pseudomonas aeruginosa ATCC 15442. Most of the new compounds showed a marked selectivity against the Gram-positive strains. Remarkably, five compounds exhibited BIC50 values against S. aureus ATCC 25923 ranging from 1.0 to 9.1 µM. The new compounds, affecting the biofilm formation without any interference on microbial growth, can be considered promising lead compounds for the development of a new class of anti-virulence agents. 相似文献
68.
Htoo Tint San Nutputsorn Chatsumpun Thaweesak Juengwatanatrakul Natapol Pornputtapong Kittisak Likhitwitayawuid Boonchoo Sritularak 《Molecules (Basel, Switzerland)》2021,26(2)
Four new phenanthrene derivatives, gastrobellinols A-D (1–4), were isolated from the methanolic extract of Gastrochilus bellinus (Rchb.f.) Kuntze, along with eleven known phenolic compounds including agrostophyllin (5), agrostophyllidin (6), coniferyl aldehyde (7), 4-hydroxybenzaldehyde (8), agrostophyllone (9), gigantol (10), 4-(methoxylmethyl)phenol (11), syringaldehyde (12), 1-(4′-hydroxybenzyl)-imbricartin (13), 6-methoxycoelonin (14), and imbricatin (15). Their structures were determined by spectroscopic methods. Each isolate was evaluated for α-glucosidase inhibitory activity. Compounds 1, 2, 3, 7, 9, 13, and 15 showed higher activity than the drug acarbose. Gastrobellinol C (3) exhibited the strongest α-glucosidase inhibition with an IC50 value of 45.92 μM. A kinetic study of 3 showed competitive inhibition on the α-glucosidase enzyme. This is the first report on the phytochemical constituents and α-glucosidase inhibitory activity of G. bellinus. 相似文献
69.
scar M. Bautista‐Aguilera Lhassane Ismaili Isabel Iriepa Daniel Diez‐Iriepa Fakher Chabchoub Jos Marco‐Contelles Marta Prez 《Chemical record (New York, N.Y.)》2021,21(1):162-174
Herein we have reviewed our recent developments for the identification of new tacrine analogues for Alzheimer's disease (AD) therapy. Tacrine, the first cholinesterase inhibitor approved for AD treatment, did not stop the progression of AD, producing only some cognitive improvements, but exhibited secondary effects mainly due to its hepatotoxicity. Thus, the drug was withdrawn from the clinics administration. Since then, many publications have described non‐hepatotoxic tacrines, and in addition, important efforts have been made to design multitarget tacrines by combining their cholinesterase inhibition profile with the modulation of other biological targets involved in AD. 相似文献
70.
Kamil J. Kuder Magdalena Kotaska Katarzyna Szczepaska Kamil Mika David Reiner-Link Holger Stark Katarzyna Kie-Kononowicz 《Molecules (Basel, Switzerland)》2021,26(8)
In an attempt to find new dual acting histamine H3 receptor (H3R) ligands, we designed a series of compounds, structurally based on previously described in our group, a highly active and selective human histamine H3 receptor (hH3R) ligand KSK63. As a result, 15 obtained compounds show moderate hH3R affinity, the best being the compound 17 (hH3R Ki = 518 nM). Docking to the histamine H3R homology model revealed two possible binding modes, with key interactions retained in both cases. In an attempt to find possible dual acting ligands, selected compounds were tested for antioxidant properties. Compound 16 (hH3R Ki = 592 nM) showed the strongest antioxidant properties at the concentration of 10−4 mol/L. It significantly reduced the amount of free radicals presenting 50–60% of ascorbic acid activity in the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay, as well as showed antioxidative properties in the ferric reducing antioxidant power (FRAP) assay. Despite the yet unknown antioxidation mechanism and moderate hH3R affinity, 16 (QD13) constitutes a starting point for the search of potential dual acting H3R ligands-promising tools for the treatment of neurological disorders associated with increased neuronal oxidative stress. 相似文献