Chemistry Research News | Stephan Scheeff

Chemistry Research News

I will present the newest insights in organic chemistry, medicinal chemistry and other related research. I will show you what I find interesting, presented in small snippets.

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

Medicinal Chemistry

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.

Sep 10, 2024

Personal Review: International Symposium on Medicinal Chemistry

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.

Sep 10, 2024

Synthesis of Quaternary Centres using Lithium Enolates in a Ru-catalysed Allylic substitution

Organic Synthesis

Synthesis of Quaternary Centres using Lithium Enolates in a Ru-catalysed Allylic substitution

The construction of quaternary centers via C-C bond formation is a significant challenge, but a new method reported in JACS, provides a promising approach to accessing these sterically crowded motifs.

Aug 24, 2024

Synthesis of Drug Libraries using Sulfamide Linker Strategy

Medicinal Chemistry

Synthesis of Drug Libraries using Sulfamide Linker Strategy

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

Aug 21, 2024

Ring Closing Alkyne Metathesis allows unified Synthesis of Strasseriolides A to D

Total Synthesis

Ring Closing Alkyne Metathesis allows unified Synthesis of Strasseriolides A to D

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

Aug 10, 2024

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

Medicinal Chemistry

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 clinical trials.

Jul 27, 2024

Biocatalytic diversification of thionucleoside analogues

Medicinal Chemistry

Biocatalytic diversification of thionucleoside analogues

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

Jul 23, 2024

Breaking the aromaticity of thiophene using a [4+3] cycloaddition

Organic Chemistry

Breaking the aromaticity of thiophene using a [4+3] cycloaddition

A novel dearomative, intramolecular [4+3]-cycloaddition of thiophenes at low temperatures yielding complex tricyclic ring systems.

Jul 19, 2024

Novel remdesivir type nucleoside analogue displays broad-spectrum antiviral activity

Medicinal Chemistry

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.

Jul 15, 2024

Structural Modifications Enhance Antibacterial Potency of Bacitracin

Medicinal Chemistry

Structural Modifications Enhance Antibacterial Potency of Bacitracin

Researchers modified the structure of the established antibiotic bacitracin, leading to a 256-fold increase in activity and potent inhibition of vancomycin-resistant strains.

Jul 13, 2024

Novel Synthesis Route to Platensilin and Analogues

Total Synthesis

Novel Synthesis Route to Platensilin and Analogues

Researchers from Shandong University in China reported the total synthesis of platensilin and platensimycin, as well as the formal synthesis of platencin in JACS, using a biomimetic approach that allowed the formation of all three natural products from a common precursor.

Jul 9, 2024

My Reading Tip of the Week: Total Synthesis of Scabrolide A by Radical Cascade

Total Synthesis

My Reading Tip of the Week: Total Synthesis of Scabrolide A by Radical Cascade

A radical cascade strategy to synthesize the complex marine natural product, Scabrolide A, is described in JACS by Pengfei Hu and coworkers.

Jun 1, 2024

My Reading Tip of the Week: Efficacy of Remdesivir ProDrugs

Medicinal Chemistry

My Reading Tip of the Week: Efficacy of Remdesivir ProDrugs

The efficacy of triphosphate formation of remdesivir is dependent on ProTide substitution. Higher levels of triphosphate in the lung are observed with ProTide prodrugs.

May 24, 2024