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Design, synthesis and insecticidal activities of novel m-diamide compounds containing n-propyl group
Design, synthesis and insecticidal activities of novel m-diamide compounds containing n-propyl group
To develop a structurally novel and efficient insecticide, a series of meta-diamide compounds incorporating n-propyl group...
Design, synthesis and antifungal study of novel 2-aryl-3,4-dihydroisoquinolin-2-ium salts containing benzoate moieties
Design, synthesis and antifungal study of novel 2-aryl-3,4-dihydroisoquinolin-2-ium salts containing benzoate moieties
To discover natural-derived fungicides, three series of 2-aryl-3,4-dihydroisoquinolinium salts (6–8) containing benz...
Synthesis and antibacterial activity of environmentally friendly sulfonium compounds
Synthesis and antibacterial activity of environmentally friendly sulfonium compounds
The abuse and overuse of antibacterial drugs have caused the increasing drug resistance of pathogenic bacteria, which thre...
Pancreatic lipase inhibitors as anti-obesity agents: a review of recent chemical scaffolds and their pancreatic lipase inhibitory potential
Pancreatic lipase inhibitors as anti-obesity agents: a review of recent chemical scaffolds and their pancreatic lipase inhibitory potential
Obesity is an excessive accumulation of fat in the body. The disease of obesity is increasing all over the world. At prese...
Design, synthesis, in vitro evaluation, and molecular dynamics simulation studies of novel coumarin-acetohydrazide Schiff base derivatives as urease enzyme inhibitors
Design, synthesis, in vitro evaluation, and molecular dynamics simulation studies of novel coumarin-acetohydrazide Schiff base derivatives as urease enzyme inhibitors
Urease inhibition, a nickel-containing metalloenzyme, is a promising approach for treating Helicobacter pylori (H. pylori)...
Development of novel triconjugates fusing melatonin/isatin/N-acylhydrazone targeting colorectal cancer: design, synthesis, biological, and in silico ADME/Tox profiling
Development of novel triconjugates fusing melatonin/isatin/N-acylhydrazone targeting colorectal cancer: design, synthesis, biological, and in silico ADME/Tox profiling
Herein, a new library of triconjugates linked melatonin with the biological active cores of isatin and N-acylhydrazone wer...
In vitro and in silico studies on α-glucosidase inhibitory properties of bioactive components from the rhizomes of Alpinia officinarum Hance
In vitro and in silico studies on α-glucosidase inhibitory properties of bioactive components from the rhizomes of Alpinia officinarum Hance
Key digestive enzymes, α-glucosidase and α-amylase, are associated with the occurrence of type 2 diabetes mellit...
Design, synthesis, and neuroprotective activity of salidroside-based dual inhibitors of selective monoamine oxidase B and amyloid-β aggregation
Design, synthesis, and neuroprotective activity of salidroside-based dual inhibitors of selective monoamine oxidase B and amyloid-β aggregation
This study focuses on the design, synthesis, and evaluation of a series of salidroside derivatives (pOBZ-1~pOBZ-11) for th...
Synthesis and anti-inflammatory activity of chromone-sulfonamide derivatives as COXs/iNOS dual-target inhibitors
Synthesis and anti-inflammatory activity of chromone-sulfonamide derivatives as COXs/iNOS dual-target inhibitors
Cyclooxygenase and inducible nitric oxide synthase are key proteins in two different pathways that produce inflammation. I...
Multivalent MMP-12 inhibitors as a valuable approach to counteract the intestinal epithelial barrier impairment and inflammation in an in vitro model mimicking intestinal high-fat exposure
Multivalent MMP-12 inhibitors as a valuable approach to counteract the intestinal epithelial barrier impairment and inflammation in an in vitro model mimicking intestinal high-fat exposure
Intestinal epithelial barrier (IEB) impairment represents a prodromal event underlying obesity and related systemic inflam...
Design, synthesis, and evaluation of benzylpiperidine-derived hydrazones as dual inhibitors of monoamine oxidases and acetylcholinesterase
Design, synthesis, and evaluation of benzylpiperidine-derived hydrazones as dual inhibitors of monoamine oxidases and acetylcholinesterase
Alzheimer’s disease (AD) is a multifaceted neurodegenerative disorder characterized by cognitive decline and memory ...
Novel alkoxy- and prenyl-xanthones derivatives as potential antidiabetic agents: Synthesis, in vitro evaluation and in silico studies
Novel alkoxy- and prenyl-xanthones derivatives as potential antidiabetic agents: Synthesis, in vitro evaluation and in silico studies
Novel alkoxy-xanthones 5, 7, 9, 10, and 10-14 were synthesized and evaluated in vitro for their ability to inhibit α-...
Synthesis, bacteria activity and molecular simulation of D-galactose-conjugated thiosemicarbazones of 3-aryl-4-formylsydnones
Synthesis, bacteria activity and molecular simulation of D-galactose-conjugated thiosemicarbazones of 3-aryl-4-formylsydnones
A series of D-galactose-conjugated substituted 4-formylsydnone thiosemicarbazones 4a-j were designed and synthesized from ...
Synthesis, characterization, and evaluation of KDM4B inhibitors to attenuate inflammatory host immune response in periodontitis
Synthesis, characterization, and evaluation of KDM4B inhibitors to attenuate inflammatory host immune response in periodontitis
Periodontal disease begins with bacterial plaque buildup in the oral cavity, inciting an inflammatory response that result...
CYP3A4 drug metabolism considerations in pediatric pharmacotherapy
CYP3A4 drug metabolism considerations in pediatric pharmacotherapy
Cytochrome P450 3A4 (CYP3A4) is a crucial enzyme involved in the Phase I metabolism of numerous medications used in clinic...
In Memory of Professor Patrick M. Woster (1955–2023): a loss to the field of medicinal chemistry
In Memory of Professor Patrick M. Woster (1955–2023): a loss to the field of medicinal chemistry
It has been a bit more than a year since Patrick M. Woster suddenly passed away in Ju...
Synthesis and biological assessment of triazolo-quinazoline carbothioamide derivatives for p38 MAP kinase inhibition: in-silico and in-vitro approaches
Synthesis and biological assessment of triazolo-quinazoline carbothioamide derivatives for p38 MAP kinase inhibition: in-silico and in-vitro approaches
A series of 4-Alkyl-5-oxo-N-(pyridin-3-yl)-4,5-dihydro [1,2,3] triazolo[1,5-a] quinazoline-3-carbothioamide compounds (8a-...
Integrating omics data for personalized medicine in treating psoriasis
Integrating omics data for personalized medicine in treating psoriasis
Psoriasis is a chronic, multifactorial skin disorder characterized by the hyperproliferation of keratinocytes and persiste...
Design, synthesis, stereochemical characterization, in vitro α-glucosidase, and α-amylase inhibition and in silico studies of novel pyrazole-hydrazide hydrazones
Design, synthesis, stereochemical characterization, in vitro α-glucosidase, and α-amylase inhibition and in silico studies of novel pyrazole-hydrazide hydrazones
In this work, a novel series of fifteen pyrazole-linked hydrazide-hydrazone derivatives (4a-o) were designed, synthesized,...
A fragment-based screen for inhibitors of Escherichia coli N5-CAIR mutase
A fragment-based screen for inhibitors of Escherichia coli N5-CAIR mutase
Although purine biosynthesis is a primary metabolic pathway, there are fundamental differences between how purines are syn...
Targeting RNA-protein interactions with small molecules: promise and therapeutic potential
Targeting RNA-protein interactions with small molecules: promise and therapeutic potential
The therapeutic potential of targeting protein-RNA interactions has not been fully explored. While several approaches to b...
α-Glucosidase inhibitory activities of aromatic compounds from the rhizomes of Alpinia galanga
α-Glucosidase inhibitory activities of aromatic compounds from the rhizomes of Alpinia galanga
Inhibition of α-glucosidase is a widely recognized approach for managing hyperglycemia, particularly postprandial glu...
Phytochemical constituents isolated from Silene popovii Schischk
Phytochemical constituents isolated from Silene popovii Schischk
In this work, with the aim to find new and biologically active natural compounds, the chemical content of the apolar and p...
Professor Stephen Neidle: A pioneer in cancer research and DNA-targeting drug discovery
Professor Stephen Neidle: A pioneer in cancer research and DNA-targeting drug discovery
This issue of Medicinal Chemistry Research is dedicated to Professor Stephen Neidle f...
A guide for asymmetric synthesis of morphine alkaloids
A guide for asymmetric synthesis of morphine alkaloids
A collection of structurally related natural compounds derived from Papaver somniferum, the opium poppy, are known as the ...
Design, synthesis and antitumor activity evaluation of benzimidazole derivatives with potent HDAC inhibitory activity
Design, synthesis and antitumor activity evaluation of benzimidazole derivatives with potent HDAC inhibitory activity
This study aims to design and synthesize novel benzimidazole histone deacetylase (HDAC) inhibitors to explore their potent...
Oligonucleotides: evolution and innovation
Oligonucleotides: evolution and innovation
Oligonucleotides, comprising single or double strands of RNA or DNA, are vital chemical compounds used in various laborato...
Inhibition of SARS-CoV-2 replication in cells by G-quadruplex ligands
Inhibition of SARS-CoV-2 replication in cells by G-quadruplex ligands
The coronavirus SARS-CoV-2 continues to spread worldwide. Dozens of compounds have been discovered based on the structure ...
Evaluation of cholinesterase enzyme inhibitory potential of dipterocarpol derivatives
Evaluation of cholinesterase enzyme inhibitory potential of dipterocarpol derivatives
Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) - are depression and neurodegenerative diseases that target e...
Review: Chemical and biological features of genus Paralemnalia soft corals
Review: Chemical and biological features of genus Paralemnalia soft corals
Marine soft corals are plentiful sources of a wide range of natural products. They include an extensive array of chemical ...
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