Design of selective COX-2 inhibitors in the (aza)indazole series. Chemistry, in vitro studies, radiochemistry and evaluations in rats of a [
Animals
Aza Compounds
/ chemical synthesis
Cyclooxygenase 2
/ metabolism
Cyclooxygenase 2 Inhibitors
/ chemical synthesis
Dose-Response Relationship, Drug
Fluorine Radioisotopes
Indazoles
/ chemical synthesis
Molecular Structure
Positron-Emission Tomography
Radioactive Tracers
Radiopharmaceuticals
/ chemical synthesis
Rats
Structure-Activity Relationship
(aza)indazoles
Cyclooxygenase
NSAID
PET
boronic ester
neuroinflammation
radiolabeling
Journal
Journal of enzyme inhibition and medicinal chemistry
ISSN: 1475-6374
Titre abrégé: J Enzyme Inhib Med Chem
Pays: England
ID NLM: 101150203
Informations de publication
Date de publication:
Dec 2019
Dec 2019
Historique:
entrez:
27
10
2018
pubmed:
27
10
2018
medline:
10
11
2018
Statut:
ppublish
Résumé
A series of novel derivatives exhibiting high affinity and selectivity towards the COX-2 enzyme in the (aza) indazole series was developed. A short synthetic route involving a bromination/arylation sequence under microwave irradiation and direct C-H activation were established in the indazole and azaindazole series respectively. In vitro assays were conducted and structural modifications were carried out on these scaffolds to furnish compound 16 which exhibited effective COX-2 inhibitory activity, with IC
Identifiants
pubmed: 30362376
doi: 10.1080/14756366.2018.1501043
pmc: PMC6211253
doi:
Substances chimiques
Aza Compounds
0
Cyclooxygenase 2 Inhibitors
0
Fluorine Radioisotopes
0
Indazoles
0
Radioactive Tracers
0
Radiopharmaceuticals
0
Cyclooxygenase 2
EC 1.14.99.1
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
1-7Références
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