Listar por tema "synthesis"
Mostrando ítems 1-20 de 30
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The architecture of hydrogen and sulfur σ-hole interactions explain differences in the inhibitory potency of C-β-D-glucopyranosyl thiazoles, imidazoles and an N-β-D glucopyranosyl tetrazole for human liver glycogen phosphorylase and offer new insights to structure-based design
(2020)C-Glucopyranosyl imidazoles, thiazoles, and an N-glucopyranosyl tetrazole were assessed in vitro and ex vivo for their inhibitory efficiency against isoforms of glycogen phosphorylase (GP; a validated pharmacological target ... -
The Circle of Friends intervention: a research synthesis
(2022)This research synthesis investigates studies that evaluated a well-known intervention, the Circle of Friends (CoF)–which seeks to promote the inclusion of socially neglected students. The aim of the review is two-fold; ... -
Curcumin derivatives as potential mosquito larvicidal agents against two mosquito vectors, culex pipiens and aedes albopictus
(2021)Vector-borne diseases have appeared or re-emerged in many Southern Europe countries making the transmission of infectious diseases by mosquitoes (vectors) one of the greatest worldwide health threats. Larvicides have been ... -
Current status and future prospects of small–molecule protein–protein interaction (PPI) inhibitors of tumor necrosis factor (TNF) and receptor activator of NF-κB ligand (RANKL)
(2018)The overexpression of Tumor Necrosis Factor (TNF) is directly related to the development of several autoimmune diseases, such as rheumatoid and psoriatic arthritis, inflammatory bowel disease, Crohn’s disease, refractory ... -
Design and Synthesis of Type-IV Inhibitors of BRAF Kinase That Block Dimerization and Overcome Paradoxical MEK/ERK Activation
(2019)Despite the clinical success of BRAF inhibitors like vemurafenib in treating metastatic melanoma, resistance has emerged through "paradoxical MEK/ERK signaling" where transactivation of one protomer occurs as a result of ... -
Design, synthesis, and biological evaluation of novel C5-modified pyrimidine ribofuranonucleosides as potential antitumor or/and antiviral agents
(2020)Background: Nucleoside analogues are well-known antitumor, antiviral, and chemotherapeutic agents. Alterations on both their sugar and the heterocyclic parts may lead to significant changes in the spectrum of their biological ... -
Discovery of Small-Molecule Inhibitors of Receptor Activator of Nuclear Factor-κB Ligand with a Superior Therapeutic Index
(2020)Receptor activator of nuclear factor-κB ligand (RANKL) constitutes the master mediator of osteoclastogenesis, while its pharmaceutical inhibition by a monoclonal antibody has been approved for the treatment of postmenopausal ... -
The Discursive Performance of Change Process in Systemic and Constructionist Therapies: A Systematic Meta-Synthesis Review of In-Session Therapy Discourse
(2021)Despite the emphasis of systemic and constructionist approaches on discourse and interaction, to date there has been no comprehensive overview of how change process is performed within in-session therapeutic dialogue. In ... -
Efficient carbon dioxide electroreduction over rationally designed heterogeneous Ag2S-Au nanocomposites
(2022)Electrochemical carbon dioxide reduction reaction (CO2RR) is regarded as an effective strategy to store abundant renewable energy and build a carbon neutral society. Gold (Au) and silver (Ag)-based catalysts for the effective ... -
Enhanced oxygen reduction and methanol oxidation reaction over self-assembled Pt-M (M = Co, Ni) nanoflowers
(2022)Herein, we introduce a facile approach to synthesize a unique class of Pt-M (M = Ni, Co) catalysts with a nanoflower structure for boosting both oxygen reduction reaction (ORR) and methanol oxidation reaction (MOR). By ... -
Glucopyranosylidene-spiro-imidazolinones, a New Ring System: Synthesis and Evaluation as Glycogen Phosphorylase Inhibitors by Enzyme Kinetics and X-ray Crystallography
(2019)Epimeric series of aryl-substituted glucopyranosylidene-spiro-imidazolinones, an unprecedented new ring system, were synthesized from the corresponding Schiff bases of O-perbenzoylated (gluculopyranosylamine)onamides by ... -
Glycogen phosphorylase as a target for type 2 diabetes: Synthetic, biochemical, structural and computational evaluation of novel N-acyl-N´-(β-D-glucopyranosyl) urea inhibitors
(2015)Glycogen phosphorylase (GP), a validated target for the development of anti-hyperglycaemic agents, has been targeted for the design of novel glycopyranosylamine inhibitors. Exploiting the two most potent inhibitors from ... -
High consistency of structure-based design and X-ray crystallography: Design, synthesis, kinetic evaluation and crystallographic binding mode determination of biphenyl-n-acyl-β-d-glucopyranosylamines as glycogen phosphorylase inhibitors
(2019)Structure-based design and synthesis of two biphenyl-N-acyl-β-D-glucopyranosylamine derivatives as well as their assessment as inhibitors of human liver glycogen phosphorylase (hlGPa, a pharmaceutical target for type 2 ... -
Highly stable cathodes for proton exchange membrane fuel cells: Novel carbon supported Au@PtNiAu concave octahedral core-shell nanocatalyst
(2022)Despite the remarkable research efforts, the lack of ideal activity and state-of-the-art electrocatalysts remains a substantial challenge for the global application of fuel cell technology. Herein, is reported the synthesis ... -
How is Systemic and Constructionist Therapy Change Process Narrated in Retrospective Accounts of Therapy? A Systematic Meta-synthesis Review
(2021)Despite the considerable potential of qualitative approaches for studying the systemic and constructionist therapy process due to shared theoretical and epistemological premises, to date there is lack of a comprehensive ... -
Magnetic nanoparticles in medical diagnostic applications: Synthesis, characterization and proteins conjugation
(2016)Background: Magnetic nanoparticles (NPs) used in biomedical applications should be discrete with small particle sizes, narrow size distribution and superparamagnetic. NPs can be tailored to target, through chemical bonds, ... -
A Meta-Epidemiological Study of Positive Results in Clinical Nutrition Research: The Good, the Bad and the Ugly of Statistically Significant Findings
(2022)Positive (statistically significant) findings are easily produced in nutrition research when specific aspects of the research design and analysis are not accounted for. To address this issue, recently, a pledge was made ... -
A multidisciplinary study of 3-(β-D-glucopyranosyl)-5-substituted-1,2,4-triazole derivatives as glycogen phosphorylase inhibitors: Computation, synthesis, crystallography and kinetics reveal new potent inhibitors
(2018)3-(β-D-Glucopyranosyl)-5-substituted-1,2,4-triazoles have been revealed as an effective scaffold for the development of potent glycogen phosphorylase (GP) inhibitors but with the potency very sensitive to the nature of the ... -
Nanomolar Inhibitors of Glycogen Phosphorylase Based on β- D -Glucosaminyl Heterocycles: A Combined Synthetic, Enzyme Kinetic, and Protein Crystallography Study
(2017)Aryl substituted 1-(β-d-glucosaminyl)-1,2,3-triazoles as well as C-β-d-glucosaminyl 1,2,4-triazoles and imidazoles were synthesized and tested as inhibitors against muscle and liver isoforms of glycogen phosphorylase (GP). ... -
A new method for synthesizing test accuracy data outperformed the bivariate method
(2021)Objectives: This study outlines the development of a new method (split component synthesis; SCS) for meta-analysis of diagnostic accuracy studies and assesses its performance against the commonly used bivariate random ...