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
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
Synthesis of Drug Libraries using Sulfamide Linker Strategy
A coupling strategy ready for use in a 96 well plate.
Aug 21, 2024
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
Novel biocatalytic method for the diversification of thionucleosides, demonstrating that enzyme-catalyzed transglycosylation can effectively facilitate nucleobase exchange.
Jul 23, 2024
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
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
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