Chalcone Library Yields Nanomolar MAO-B Inhibitors for Neurodegeneration
Researchers have identified a morpholine-substituted chalcone, TC12, that inhibits monoamine oxidase B at 11 nanomolar with over 3,600-fold selectivity and ...
Tag: medicinal chemistry
Chemists Turn CO2, Nitrite and Aldehydes Into Valuable Amino Acids Using Only Electricity
Yale chemists have developed a two-step electrosynthesis that converts carbon dioxide, nitrite and aromatic aldehydes into valuable arylglycine amino acids ...
AI Chemist Learns to Edit Molecules Into Makeable Medicines
Researchers at Peking University have developed SynCraft, a framework that uses large language models to predict precise atom-level edit sequences ...
Engineered Cytisine Derivative Disrupts Redox Balance to Kill Lung Cancer Cells
Researchers engineered a thiourea-bridged cytisine derivative, YU-C-ThioU-9, that overwhelms the antioxidant defenses of lung cancer cells by disrupting Nrf2-Keap1 and ...
Electricity Powers a Greener Route to Deuterium-Labeled Antioxidant Molecules
Chemists have developed an electrochemical three-component cascade that installs trideuteromethylthio groups onto enaminones, yielding compounds that can protect cells from ...
AI-designed molecules plus expert chemistry yield nanomolar tyrosinase inhibitors
A reinforcement learning model that designs synthetically accessible molecules from scratch, combined with expert medicinal chemistry, produced a tyrosinase inhibitor ...
Nickel Catalyst Alkylates Drug-Like Rings at Mild Temperatures
Scripps Research chemists have developed a nickel-catalysed, sulfonylhydrazide-based C–H alkylation that attaches alkyl groups to arenes and heteroarenes below 50 ...
Copper Catalyst Stays in Balance: KAIST Ligand Strategy Unlocks Stubborn Alkyl Chlorides for Drug-Like Molecules
KAIST chemists used a cyclopropenimine ligand to balance radical generation and copper catalyst regeneration, enabling difficult radical cyclizations of tertiary ...
PROTACs Move From Lab Concept to Clinical Reality in Targeted Protein Degradation
A new comprehensive review in Discover Chemistry details how PROTACs have evolved from a mechanistic concept into clinically advanced degraders ...
Phosphorus-Powered Pyrazoles Show Potent Antimicrobial Activity Against E. coli
Chemists have synthesized a series of N-phosphorylated 5-aminopyrazoles that show promising antibacterial activity, with one thiophosphorylated derivative approaching the potency ...
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Mothers who receive childcare support from maternal grandparents show more parental warmth, finds NTU Singapore study
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University of Seville Breaks 120-Year-Old Mystery, Revises a Key Einstein Concept
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Bee body mass, pathogens and local climate influence heat tolerance
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Researchers record first-ever images and data of a shark experiencing a boat strike
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Groundbreaking Clinical Trial Reveals Lubiprostone Enhances Kidney Function
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