2-(4-Methylsulfonylphenyl)pyrimidines as Prospective Radioligands for Imaging Cyclooxygenase-2 with PET—Synthesis, Triage, and Radiolabeling

• Published in: Molecules (Basel, Switzerland) Vol. 23; no. 11; p. 2850
• Main Authors: Cortes-Salva, Michelle Y., Shrestha, Stal, Singh, Prachi, Morse, Cheryl L., Jenko, Kimberly J., Montero Santamaria, Jose A., Zoghbi, Sami S., Innis, Robert B., Pike, Victor W.
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 02.11.2018; MDPI
• Subjects: Alzheimer's disease; Carbon; carbon-11; COX-2; Drug development; Enzymes; Fluorine; fluorine-18; Inflammation; Labeling; Ligands; Nonsteroidal anti-inflammatory drugs; radioligand; radioligand; carbon-11; fluorine-18; COX-2

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 in...