Results 161 to 170 of about 126,317 (283)
This paper by Kollár et al. reports a covalent fragment linking study against the SARS‐CoV‐2 main protease (3CLPro). Beginning with inactive fragment hits, the application of rational linker design enabled the generation of reversible covalent inhibitors exhibiting low micromolar potency. The study details some general limitations and best practices of
Levente Kollár +8 more
wiley +1 more source
Mixed‐Functionalized Acylgermanes Result in Wavelength‐Controlled Fragmentation
Selective radical generation from PEG‐acylgermanes is achieved by controlling the used wavelength. Distinct aryl‐carbonyl units undergo wavelength‐dependent α‐cleavage, producing radicals with different reactivities. UV/Vis, TD‐DFT, and photo‐CIDNP spectroscopy confirm that small adjustments in light input directly dictate radical identity and ...
André Culum +6 more
wiley +2 more sources
Chemical Ligation of Backbone N‐hydroxylated Peptides
Peptide backbone N‐hydroxylation enables sequence‐agnostic fragment ligation via hydroxamate O‐acyl capture and O→N acyl transfer in water. Broad tolerance of sterically demanding nucleophilic residues is observed, and reductive N─O cleavage restores the native amide bond.
Natalia Cano‐Sampaio +1 more
wiley +1 more source
Push–Pull Ynamines and Push–Pull Ynamides: Synthesis, Structure, Reactivity, and Application
Push–pull ynamines and push–pull ynamides, which carry an EWG and an amino or amido group as EDG, are highly interesting classes of EDG‐EWG alkynes that have been intensively studied due to their exceptional reactivity. In this review, the synthesis, structure, reactivity, and application of push–pull ynamines, push–pull ynecarbamates, push–pull ...
Hans‐Joachim Gais
wiley +1 more source
Alkyltransferase Ribozyme for Site‐Specific N4‐Cytidine Alkylation
CSAR is the first ribozyme that catalyzes direct alkylation of an exocyclic amino group of an RNA nucleobase. The ribozyme was isolated as a self‐labeling catalyst from an in vitro selection library and engineered into a trans‐active ribozyme that catalyzes the transfer of a benzyl group from an O6‐modifed guanine to the N4 amino group of a specific ...
Evgeniia Dorinova +2 more
wiley +2 more sources
From Brewing to Plastic Degradation: Uncovering the Polyurethanase Potential of <i>R. chinensis</i> Lipase through Atomistic Simulations. [PDF]
de Sousa Batista V +2 more
europepmc +1 more source
1,2‐Diazetidines − Structure, Synthesis, and Functionalization
1,2‐Diazetidines are saturated four‐membered heterocycles featuring two adjacent nitrogen atoms. Despite recent advances in their synthesis and promising potential in medicinal chemistry, the chemistry of these cyclic hydrazines remains underexplored.
Stefan Roesner
wiley +1 more source
Proximity-driven acceleration of challenging solid-phase peptide couplings. [PDF]
Parker J +5 more
europepmc +1 more source
Combining enhanced permeability strategies with (2‐pyridyl)methylene substitution in the sulbactam scaffold led to a novel β‐lactamase inhibitor to combat β‐lactamase‐mediated resistance to β‐lactam antibiotics. The studies presented highlight the potential of compound 3 as a next‐generation β‐lactamase inhibitor for combating infections caused by ...
Diana Rodríguez +4 more
wiley +1 more source
Multi-step biocatalytic strategy to produce a library of original xylosides with various ester functions for cosmetic applications. [PDF]
Jolly E +3 more
europepmc +1 more source

