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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 ...
Thiophene ring-opening reactions. Part VII: synthesis and antitumor, anti-inflammatory, and antioxidant properties of 1,3,4‒thiadiazoline‒6-sulfanylthiopyran-4(1H)-one hybrids
Thiophene ring-opening reactions. Part VII: synthesis and antitumor, anti-inflammatory, and antioxidant properties of 1,3,4‒thiadiazoline‒6-sulfanylthiopyran-4(1H)-one hybrids
The reaction of N′’(aryl)benzothiohydrazides with 2-chloro-6-((substituted)amino)-3-nitro-4-oxo-4H-thieno[2,3-...
The versatile NDI-based compounds: emerging anticancer and antimicrobial agents
The versatile NDI-based compounds: emerging anticancer and antimicrobial agents
G-quadruplexes (G4s) are non-canonical nucleic acid structures present in guanine-rich sequences, notably within cancer-as...
Investigating novel tubulin polymerization inhibitors: design, synthesis, LC/MS cellular permeability, in silico studies, and in vitro assessment
Investigating novel tubulin polymerization inhibitors: design, synthesis, LC/MS cellular permeability, in silico studies, and in vitro assessment
In this study, chalcones 5, and 6 and pyrazolines 7, and 8 were designed and synthesized as combrestatin A-4 (CA-4) analog...
Monoamine oxidase inhibition by thiazole derivatives substituted with the benzenesulfonamide moiety
Monoamine oxidase inhibition by thiazole derivatives substituted with the benzenesulfonamide moiety
Based on a report that 1,3,4-oxadiazol-2-ylbenzenesulfonamides act as inhibitors of monoamine oxidase B (MAO-B), the prese...
Design and synthesis of aminothiazole-benzazole based amide: antiproliferative, antimigration activity and molecular docking studies
Design and synthesis of aminothiazole-benzazole based amide: antiproliferative, antimigration activity and molecular docking studies
In this study, we synthesized a series of amide-functionalized aminothiazole-benzazole analogs for potential application i...
Design of novel benzimidazole-propane hydrazide derivatives as α-glucosidase and α-amylase inhibitors: in vitro and in silico studies
Design of novel benzimidazole-propane hydrazide derivatives as α-glucosidase and α-amylase inhibitors: in vitro and in silico studies
A new series of benzimidazole-propane hydrazide derivatives 9a-k were designed, synthesized, and evaluated for their inhib...
Triphenylphosphonium (TPP) conjugates of 1,2,3-triazolyl nucleoside analogues. Synthesis, cytotoxicity and antimicrobial activity
Triphenylphosphonium (TPP) conjugates of 1,2,3-triazolyl nucleoside analogues. Synthesis, cytotoxicity and antimicrobial activity
A series of new triphenylphosphonium (TPP) conjugates of 1,2,3-triazolyl nucleoside analogues were synthesised by coupling...
Synthesis of the dibenzylbutane lignan LCA derivatives and evaluation of their anti-inflammatory activities
Synthesis of the dibenzylbutane lignan LCA derivatives and evaluation of their anti-inflammatory activities
The roots of Litsea cubeba (Lour.) Pers have been used for the treatment of rheumatism. We previously extracted and isolat...
Synthesis and in vitro antiproliferative evaluation of novel drimane oxepinyl triazoles from labdane diterpene sclareol
Synthesis and in vitro antiproliferative evaluation of novel drimane oxepinyl triazoles from labdane diterpene sclareol
A series of new oxepinyl triazoles were synthesized using labdane diterpene sclareol as a template. The synthesis process ...
Design, synthesis, and evaluation of antitumor activity of quinazoline derivatives containing different terminal segments of basic amine groups
Design, synthesis, and evaluation of antitumor activity of quinazoline derivatives containing different terminal segments of basic amine groups
In this study, we designed and synthesized 41 quinazoline derivatives with different base amine termini. Compound 15n show...
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