ArticleMolecules (Basel, Switzerland)2018
2-(4-Methylsulfonylphenyl)pyrimidines as Prospective Radioligands for Imaging Cyclooxygenase-2 with PET-Synthesis, Triage, and Radiolabeling.
Article in Molecules (Basel, Switzerland), 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed, 19 citations in OpenAlex.
- PET measurement of cyclooxygenase-2 using a novel radioligand: upregulation in primate neuroinflammation and first-in-human study.Journal of neuroinflammation · 2020Trial
- An Approach Toward Radioiodination and Radiopharmacological Evaluation of a Carborane-Containing Analog of Indomethacin.Molecules (Basel, Switzerland) · 2026Article
- PET Quantification in Healthy Humans of Cyclooxygenase-2, a Potential Biomarker of Neuroinflammation.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2025Article
- Design, Synthesis, and Biological Evaluation of Novel Phenoxy Acetic Acid Derivatives as Selective COX-2 Inhibitors Coupled with Comprehensive Bio-Pharmacological Inquiry, Histopathological Profiling, and Toxicological Scrutiny.Molecules (Basel, Switzerland) · 2024Article
- Fluorine-18 Labelled Radioligands for PET Imaging of Cyclooxygenase-2.Molecules (Basel, Switzerland) · 2022Review
- Repurposing [Molecular imaging and biology · 2022Article
- Cyclooxygenases as Potential PET Imaging Biomarkers to Explore Neuroinflammation in Dementia.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2022Review
- The Repertoire of Small-Molecule PET Probes for Neuroinflammation Imaging: Challenges and Opportunities beyond TSPO.Journal of medicinal chemistry · 2021Review
- NRM 2021 Abstract Booklet.Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2021Article
- Neuroinflammation in psychiatric disorders: PET imaging and promising new targets.The lancet. Psychiatry · 2020Review
- Molecular imaging of multiple sclerosis: from the clinical demand to novel radiotracers.EJNMMI radiopharmacy and chemistry · 2019Review
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Authors and funding
9 authors at 1 institution in 1 country.
Funding
Abstract
Cyclooxygenase 2 (COX-2) is an inducible enzyme responsible for the conversion of arachidonic acid into the prostaglandins, PGG2 and PGH2. Expression of this enzyme increases in inflammation. Therefore, the development of probes for imaging COX-2 with positron emission tomography (PET) has gained interest because they could be useful for the study of inflammation in vivo, and for aiding anti-inflammatory drug development targeting COX-2. Nonetheless, effective PET radioligands are still lacking. We synthesized eleven COX-2 inhibitors based on a 2(4-methylsulfonylphenyl)pyrimidine core from which we selected three as prospective PET radioligands based on desirable factors, such as high inhibitory potency for COX-2, very low inhibitory potency for COX-1, moderate lipophilicity, and amenability to labeling with a positronemitter. These inhibitors, namely 6-methoxy-2-(4-(methylsulfonyl)phenyl-
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.