Research developments in the syntheses, anti-inflammatory activities and structure–activity relationships of pyrimidines

H ur Rashid, MAU Martines, AP Duarte, J Jorge… - RSC …, 2021 - pubs.rsc.org
Pyrimidines are aromatic heterocyclic compounds that contain two nitrogen atoms at
positions 1 and 3 of the six-membered ring. Numerous natural and synthetic pyrimidines are …

Fluorine-18 labelled building blocks for PET tracer synthesis

D Van Der Born, A Pees, AJ Poot, RVA Orru… - Chemical Society …, 2017 - pubs.rsc.org
Positron emission tomography (PET) is an important driver for present day healthcare.
Fluorine-18 is the most widely used radioisotope for PET imaging and a thorough overview …

Selective cyclooxygenase-2 inhibitors: A review of recent chemical scaffolds with promising anti-inflammatory and COX-2 inhibitory activities

NA Mohsin, M Irfan - Medicinal Chemistry Research, 2020 - Springer
Abstract Selective cyclooxygenase-2 (COX-2) inhibitors have exhibited notable medicinal
importance. In recent years, the discovery of new anti-inflammatory agents as selective COX …

New pyrimidine-5-carbonitriles as COX-2 inhibitors: design, synthesis, anticancer screening, molecular docking, and in silico ADME profile studies

HA Al-Ghulikah, SA El-Sebaey, AKA Bass… - Molecules, 2022 - mdpi.com
Two series of cyanopyrimidine hybrids were synthesized bearing either benzo [d] imidazole,
benzo [d] oxazole, benzo [d] thiazole, and benzo [b] thiophene derivatives via methylene …

Design, synthesis and evaluation in an LPS rodent model of neuroinflammation of a novel 18F-labelled PET tracer targeting P2X7

ER Fantoni, D Dal Ben, S Falzoni, F Di Virgilio… - EJNMMI research, 2017 - Springer
Abstract Background The P2X7 receptor has been shown to play a fundamental role in the
initiation and sustenance of the inflammatory cascade. The development of a novel fluorine …

Radiotracers for Imaging of Inflammatory Biomarkers TSPO and COX-2 in the Brain and in the Periphery

BC Uzuegbunam, C Rummel, D Librizzi… - International Journal of …, 2023 - mdpi.com
Inflammation involves the activation of innate immune cells and is believed to play an
important role in the development and progression of both infectious and non-infectious …

Design, synthesis, biological evaluation, and molecular docking of some new Thieno [2, 3-d] pyrimidine derivatives

MS Tolba, AM Sayed, M Sayed, M Ahmed - Journal of Molecular Structure, 2021 - Elsevier
Due to the biological importance of thienopyrimidine derivatives, we present here a synthetic
way for the design of new thienopyrimidines (2‒11) using the precursor 2-(4-Oxo-9-phenyl …

Molecular basis for nonspecificity of nonsteroidal anti-inflammatory drugs (NSAIDs)

AK Dwivedi, V Gurjar, S Kumar, N Singh - Drug Discovery Today, 2015 - Elsevier
Highlights•Structural analysis of protein target complexes with NSAIDs is reported.•Atomic
details of the molecular interactions are described.•Target proteins are divided into three …

PET imaging of cyclooxygenase-2 (COX-2) in a pre-clinical colorectal cancer model

O Tietz, M Wuest, A Marshall, D Glubrecht, I Hamann… - EJNMMI research, 2016 - Springer
Abstract Background Cyclooxygenase-2 (COX-2) is the inducible isoform of the
cyclooxygenase enzyme family. COX-2 is involved in tumor development and progression …

Design, Synthesis, and Evaluation of an 18F‐Labeled Radiotracer Based on Celecoxib–NBD for Positron Emission Tomography (PET) Imaging of Cyclooxygenase‐2 …

J Kaur, O Tietz, A Bhardwaj, A Marshall, J Way… - …, 2015 - Wiley Online Library
A series of novel fluorine‐containing cyclooxygenase‐2 (COX‐2) inhibitors was designed
and synthesized based on the previously reported fluorescent COX‐2 imaging agent …