Journal of medicinal chemistry, 2005-05, Vol.48 (9), p.3428-3432
2005
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Details
- Autor(en) / Beteiligte
- Titel
- 1,5-Diarylpyrrole-3-acetic Acids and Esters as Novel Classes of Potent and Highly Selective Cyclooxygenase-2 Inhibitors
- Ist Teil von
- Journal of medicinal chemistry, 2005-05, Vol.48 (9), p.3428-3432
- Ort / Verlag
- Washington, DC: American Chemical Society
- Erscheinungsjahr
- 2005
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- A small set of substituted 1,5-diarylpyrrole-3-acetic and -glyoxylic acid derivatives have been synthesized, and their cyclooxygenase (COX-1 and COX-2) inhibiting properties have been evaluated. Some compounds proved to be highly selective COX-2 inhibitors, and their affinity data have been rationalized through docking simulations in terms of interactions with a crystallographic model of the COX-2 binding site.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0022-2623eISSN: 1520-4804DOI: 10.1021/jm049121qTitel-ID: cdi_proquest_miscellaneous_67793238
- Format
- –
- Schlagworte
- Acetates - chemical synthesis, Acetates - chemistry, Acetates - pharmacology, Animals, Binding Sites, Biological and medical sciences, Bones, joints and connective tissue. Antiinflammatory agents, Cell Line, Cyclooxygenase 1, Cyclooxygenase 2, Cyclooxygenase 2 Inhibitors, Cyclooxygenase Inhibitors - chemical synthesis, Cyclooxygenase Inhibitors - chemistry, Cyclooxygenase Inhibitors - pharmacology, Esters - chemical synthesis, Esters - chemistry, Esters - pharmacology, Medical sciences, Membrane Proteins, Mice, Models, Molecular, Pharmacology. Drug treatments, Prostaglandin-Endoperoxide Synthases - chemistry, Prostaglandin-Endoperoxide Synthases - metabolism, Pyrroles - chemical synthesis, Pyrroles - chemistry, Pyrroles - pharmacology