Results 121 to 130 of about 53,373 (308)
Background: Janus kinase (JAK) inhibitors alleviate pruritus and clinical signs of canine atopic dermatitis (cAD). Objective: To confirm the optimal dosing regimen of atinvicitinib, a second‐generation highly selective inhibitor of JAK1 in dogs. Conclusions and Clinical Relevance: Once‐daily atinvicitinib was safe, well‐tolerated and effective at ...
Faris Jirjis +6 more
wiley +1 more source
Development of Radioiodinated Tetrahydropyrazolopyridine Inhibitors Targeting mIDH
Iodinated tetrahydropyrazolopyridine ligands show enhanced potency and selectivity for mutant IDH1 compared with their fluorinated counterparts and can be efficiently radiolabeled with I‐125, supporting the basis for further evaluation as mIDH1‐targeting radiotheranostic candidates.
Sarandeep Kaur +7 more
wiley +1 more source
Synthesis of ferrocenyl substituted pyrazoles
Pyrazoles have been studied for over a century as an important class of heterocyclic compounds and continue to attract considerable interest due to the broad range of biological activities they possess.
MERAL GÖRMEN
core
Can a single element help address the multifactorial nature of ALS? Boron‐containing compounds combine responsiveness to reactive oxygen species (ROS), neuroprotective activity, and favorable pharmacological properties, offering a distinctive framework for disease modification in a complex disease like ALS.
Nitesh Sanghai +5 more
wiley +1 more source
1,2‐Bis(boronate) Arenes by Borylation Directed Borylation
Boron electrophiles derived from tetrabromo‐pyrazaboles and AlCl3 affect the regioselective vicinal double C–H borylation of a range of arenes and polycyclic aromatic hydrocarbons (PAHs). A subsequent pinacol installation step then affords the vicinal bis‐boronate ester‐substituted arene/PAH.
Anna V. Schellbach +4 more
wiley +2 more sources
Regioselective Diversification of Aminopyrazoles via Ir‐Catalyzed C─H Borylation
Aminopyrazoles, an important bioactive pharmacophore, are typically accessed inefficiently through de novo syntheses that yield isomeric mixtures of 3‐ and 5‐substituted derivatives. To address this challenge, we have elaborated readily available 3‐ and 5‐aminopyrazole fragments using Ir C─H borylation, regioselectively furnishing boronates for ...
Jay S. Wright +9 more
wiley +1 more source
Small‐Molecule Kinase Inhibitors Modulating Circadian Rhythms
ABSTRACT The circadian clock mechanism generates 24‐h rhythms crucial for regulating various physiological processes, and its dysregulation has been implicated in numerous diseases. In cells, the circadian clock operates through a transcriptional‐translational feedback loop, where phosphorylation plays a pivotal role in maintaining accurate circadian ...
Irene Castellino +3 more
wiley +1 more source
Pyrazoles are important heterocyclic compounds with a broad range of biological activities. A new procedure toward tri- or tetrasubstituted pyrazoles has been developed, via a one-pot gold catalyzed synthesis from hydrazines with alkynyl aldehydes or ...
Stevens, Christian +11 more
core +1 more source
Experimental setup for dsRNA feeding in Brassicogethes aeneus to evaluate the effect of a synthetic polymer nanocarrier on RNAi efficiency. The experiment assessed whether the nanocarrier enhances RNAi after oral dsRNA delivery. (a) Stability of dsRNA–nanocarrier complexes was tested in simulated gut conditions. (b) Gene expression of αCOP and dre4 was
Triin Kallavus +13 more
wiley +1 more source
Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt
Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown +2 more
wiley +1 more source

