AIMC Topic: Pyrazoles

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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...

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...

Machine Learning of Global Phosphoproteomic Profiles Enables Discrimination of Direct versus Indirect Kinase Substrates.

Molecular & cellular proteomics : MCP
Mass spectrometry allows quantification of tens of thousands of phosphorylation sites from minute amounts of cellular material. Despite this wealth of information, our understanding of phosphorylation-based signaling is limited, in part because it is...

Design, synthesis, and bioactivities of novel oxadiazole-substituted pyrazole oximes.

Bioorganic & medicinal chemistry letters
A series of novel pyrazole oxime derivatives containing a substituted oxadiazole group were designed and synthesized. The bioassay results indicated that some title compounds displayed good acaricidal and insecticidal activities against Tetranychus c...

HPLC-UV method for simultaneous determination of MK-1775 and AZD-7762 in both acetonitrile-aqueous solution and mouse plasma.

Journal of chromatography. B, Analytical technologies in the biomedical and life sciences
A sensitive and precise method is described for the simultaneous determination of two small molecule kinase inhibitors: MK-1775 (MK) and AZD-7762 (AZD), in acetonitrile (ACN)-aqueous solution and in mouse plasma. A Nova-Pak C18 reversed phase column ...

Synthesis and antimicrobial studies of novel derivatives of 4-(4-formyl-3-phenyl-1H-pyrazol-1-yl)benzoic acid as potent anti-Acinetobacter baumannii agents.

Bioorganic & medicinal chemistry letters
Microbial resistance to antibiotics is a global concern. The World Health Organization (WHO) has identified antimicrobial resistance as one the three greatest threats for human beings in the 21st century. Without urgent and coordinated action, the wo...

Exposure to fipronil elevates systolic blood pressure and disturbs related biomarkers in plasma of rats.

Environmental toxicology and pharmacology
Recent reports show that fipronil affects non-target organisms, including environmental species populations and potentially humans. We aimed to examine if fipronil exposure affects the systolic blood pressure and related biomarkers. Thus, fipronil wa...