Results 161 to 170 of about 126,317 (283)

Fragment‐Based Design of Targeted Covalent Inhibitors: The Scope and Limitation of Linking Approaches

open access: yesChemMedChem, Volume 21, Issue 10, 27 May 2026.
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

open access: yesAngewandte Chemie, Volume 138, Issue 20, 11 May 2026.
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

open access: yesChemistry – A European Journal, Volume 32, Issue 19, 22 May 2026.
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

open access: yesEuropean Journal of Organic Chemistry, Volume 29, Issue 19, 22 May 2026.
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

open access: yesAngewandte Chemie, Volume 138, Issue 20, 11 May 2026.
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

1,2‐Diazetidines − Structure, Synthesis, and Functionalization

open access: yesEuropean Journal of Organic Chemistry, Volume 29, Issue 19, 22 May 2026.
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]

open access: yesProc Natl Acad Sci U S A
Parker J   +5 more
europepmc   +1 more source

Zwitterionic Penicillin‐Derived Sulfone Inhibitor for Combating β‐Lactamase‐Mediated Antibiotic Resistance

open access: yesChemMedChem, Volume 21, Issue 9, 14 May 2026.
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

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