Medicinal Chemistry

Carbohydrate‐based drug discovery: Synthetic strategies and clinical applications

Carbohydrates are integral to drug discovery, serving as versatile templates for the development of small‐molecule therapeutics. However, their success in antiviral, anticancer, …

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Stephan Scheeff
Antiviral profiling and cellular activation of carbobicyclic nucleoside analogues featured image

Antiviral profiling and cellular activation of carbobicyclic nucleoside analogues

Nucleoside analogues are important antiviral and anticancer agents. In this study, we investigated a new class of nucleoside analogues built on a synthetically accessible …

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Stephan Scheeff

Ligand-directed self-assembling chimeras for targeted protein O-GlcNAcylation

Precise control of protein-specific O-GlcNAcylation in cells remains a major challenge. Chemically induced proximity (CIP) offers a promising path forward, but its application to …

zhihao-guo

Lactone-to-lactam editing alters the pharmacology of bilobalide

Precise transformations of natural products (NPs) can fine-tune their physicochemical properties while preserving inherently complex and evolutionarily optimized parent scaffolds. …

xiaoding-jiang
Personal Review: International Symposium on Medicinal Chemistry featured image

Personal Review: International Symposium on Medicinal Chemistry

Synthesis of stasseriolide natural products and their analogues using a ring-closing alkyne metathesis by Alois Fürstner and his team.

Macrocycles can lock the Conformation of Drug Candidates and enhance their Activity featured image

Macrocycles can lock the Conformation of Drug Candidates and enhance their Activity

Macrocycles can improve the conformation, biological activity, selectivity, ADME properties, and target affinity of small-molecule drug candidates.

Synthesis of Drug Libraries using Sulfamide Linker Strategy featured image

Synthesis of Drug Libraries using Sulfamide Linker Strategy

A coupling strategy ready for use in a 96 well plate.

Pfizer's Second-Generation SARS-CoV-2 Protease Inhibitor featured image

Pfizer's Second-Generation SARS-CoV-2 Protease Inhibitor

Researchers from Pfizer have developed a structurally-optimized SARS-CoV-2 main protease inhibitor with improved metabolic stability compared to nirmatrelvir which is now in …

Biocatalytic diversification of thionucleoside analogues featured image

Biocatalytic diversification of thionucleoside analogues

Novel biocatalytic method for the diversification of thionucleosides, demonstrating that enzyme-catalyzed transglycosylation can effectively facilitate nucleobase exchange.

Novel remdesivir type nucleoside analogue displays broad-spectrum antiviral activity featured image

Novel remdesivir type nucleoside analogue displays broad-spectrum antiviral activity

The development of a novel 4'-CN remdesivir-type nucleoside analogue demonstrating the potential of 4-aza-7,9-dideazaadenosine nucleoside analogues to exhibit antiviral activity.