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Pyrazoles

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Factor Xa inhibitors in clinical practice: Comparison of pharmacokinetic profiles.

Drug metabolism and pharmacokinetics
BACKGROUND: The anticoagulant actions of oral direct factor Xa (FXa) inhibitors can be inferred from their observed plasma concentrations; however, the steady-state pharmacokinetics (PK) of different FXa inhibitors have not been compared in clinicall...

A novel electrochemiluminescent biosensor based on resonance energy transfer between poly(9,9-di-n-octylfluorenyl-2,7-diyl) and 3,4,9,10-perylenetetracar-boxylic acid for insulin detection.

Biosensors & bioelectronics
An electrochemiluminescencent (ECL) biosensor was designed for the determination of insulin using a novel ECL resonance energy transfer (ECL-RET) strategy. In this strategy, carboxyl poly(9,9-dioctyfluorenyl-2,7-diyl) dots (PFO dots) were worked as E...

Label-Free Quantification of Pharmacokinetics in Skin with Stimulated Raman Scattering Microscopy and Deep Learning.

The Journal of investigative dermatology
The treatment of inflammatory skin conditions relies on a deep understanding of how drugs and tissue behave and interact. Although numerous methods have been developed that aim to follow and quantify topical drug pharmacokinetics, these tools can com...

Pharmacokinetics of Eltrombopag in Healthy Chinese Subjects and Effect of Sex and Genetic Polymorphism on its Pharmacokinetic and Pharmacodynamic Variability.

European journal of drug metabolism and pharmacokinetics
BACKGROUND AND OBJECTIVE: Eltrombopag is the first oral, small-molecule, non-peptide thrombopoietin receptor agonist for the treatment of idiopathic thrombocytopenic purpura. This study investigated the pharmacokinetics of eltrombopag in healthy Chin...

Reduced response to regadenoson with increased weight: An artificial intelligence-based quantitative myocardial perfusion study.

Journal of cardiovascular magnetic resonance : official journal of the Society for Cardiovascular Magnetic Resonance
BACKGROUND: There is conflicting evidence regarding the response to a fixed dose of regadenoson in patients with high body weight. The aim of this study was to evaluate the effectiveness of regadenoson in patients with varying body weights using nove...

A deep-learning model for predicting tyrosine kinase inhibitor response from histology in gastrointestinal stromal tumor.

The Journal of pathology
Over 90% of gastrointestinal stromal tumors (GISTs) harbor mutations in KIT or PDGFRA that can predict response to tyrosine kinase inhibitor (TKI) therapies, as recommended by NCCN (National Comprehensive Cancer Network) guidelines. However, gene seq...

Rational design and synthesis of pyrazole derivatives as potential SARS-CoV-2 M inhibitors: An integrated approach merging combinatorial chemistry, molecular docking, and deep learning.

Bioorganic & medicinal chemistry
The global impact of SARS-CoV-2 has highlighted the urgent need for novel antiviral therapies. This study integrates combinatorial chemistry, molecular docking, and deep learning to design, evaluate and synthesize new pyrazole derivatives as potentia...