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
Macrocycles can improve the conformation, biological activity, selectivity, ADME properties, and target affinity of small-molecule drug candidates.
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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 …
Synthesis of Drug Libraries using Sulfamide Linker Strategy
A coupling strategy ready for use in a 96 well plate.
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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.
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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 …
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Biocatalytic diversification of thionucleoside analogues
Novel biocatalytic method for the diversification of thionucleosides, demonstrating that enzyme-catalyzed transglycosylation can effectively facilitate nucleobase exchange.
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![Breaking the aromaticity of thiophene using a [4+3] cycloaddition featured image](/post/thiophene-angew-2024/featured_hu_950411bbaf1d50d7.webp)
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.
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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.
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.