Allosteric Inhibitors of SARS‐CoV‐2 RNA‐Dependent RNA Polymerase Based on N,N′‐Diphenylurea
Inhibitors of SARS‐CoV‐2 RdRp activity based on N,N′‐diphenylurea scaffold have been identified. Several compounds exhibit residual activity (RA) below 50% in an enzymatic assay (at 10 µM concentration) and improved aqueous solubility compared to the previously reported series of inhibitors.
Artem Chayka +11 more
wiley +1 more source
Is There More to Magic Mushrooms than Psilocybin? [PDF]
Johnson-Groh M.
europepmc +1 more source
Investigating the Ligand‐Binding Properties of N‐arylbenzimidazoles as Novel Elastase Inhibitors
A series of novel N‐[(3,5‐dimethylphenyl)methyl]‐1H‐benzimidazole derivatives is designed, synthesized, and evaluated for inhibitory activity against elastase. Several compounds demonstrate an antielastase activity, including the N‐(2‐bromophenyl)‐2‐(6‐chloro‐1‐(3,5‐dimethylbenzyl)‐1H‐benzo[d]imidazol‐2‐ylthio)acetamide, showing the greatest potency ...
Giovanna Pitasi +6 more
wiley +1 more source
From international guidelines to practice: a multimethod evaluation of <i>BMJ</i> Rapid Recommendations focusing on suitability for adaptation and implementation. [PDF]
Seterelv SS +6 more
europepmc +1 more source
A Facile Protocol for C(sp2)–C(sp3) Bond Formation Reactions Toward Functionalized E3 Ligase Ligands
A robust C(sp2)–C(sp3) decarboxylative coupling strategy enables access to new CRBN ligands and degraders with improved physicochemical properties. This synthetic approach is expanding the chemical space beyond C(sp2)–N linkages, fine‐tuning proteolysis‐targeting chimera activities and unlocking previously inaccessible degrader chemotypes.
Anita Maksutova +15 more
wiley +1 more source
Eyelid Arteriovenous Malformation With Orbital Fistula: Literature Review and Case Report. [PDF]
Ludovico I +4 more
europepmc +1 more source
Searching for Novel Antiviral Agents as COVID19 Treatments: Guanidino Diaryl Thioureas
Structure of the "hit‐compound" found and the proposed interaction with the active site of the TMPRSS2 protease, involving a reversible mechanism of action, are shown. The COVID‐19 pandemic highlighted the urgent need for effective antiviral treatments targeting SARS‐CoV‐2.
Marco Minneci +6 more
wiley +1 more source
Aroma Profiling and Sensory Association of Six Raspberry Cultivars Using HS-SPME/GC-MS and OPLS-HDA. [PDF]
Ljujić J +7 more
europepmc +1 more source
Multi-trait ridge regression BLUP with <i>de novo</i> GWAS improves genomic prediction for haploid induction ability of haploid inducers in maize. [PDF]
Chen YR, Frei UK, Lübberstedt T.
europepmc +1 more source

