4,5-Diaryloxazole inhibitors of cyclooxygenase-2 (COX-2)
| العنوان: | 4,5-Diaryloxazole inhibitors of cyclooxygenase-2 (COX-2) |
|---|---|
| المؤلفون: | Jeffery S. Carter, John J. Talley, Karen Seibert, Stephen R. Bertenshaw, D. Joseph Rogier, Carol M. Koboldt, Graneto Matthew J, David L. Brown, Ben S. Zweifel, Jaime L. Masferrer, Bryan H. Norman |
| المصدر: | Medicinal Research Reviews. 19:199-208 |
| بيانات النشر: | Wiley, 1999. |
| سنة النشر: | 1999 |
| مصطلحات موضوعية: | Pharmacology, chemistry.chemical_classification, biology, Chemistry, medicine.drug_class, Stereochemistry, Biological activity, In vitro, Anti-inflammatory, Enzyme, Biochemistry, Enzyme inhibitor, In vivo, Drug Discovery, biology.protein, medicine, Molecular Medicine, Cyclooxygenase, Selectivity |
| الوصف: | A series of methysulfonyl or sulfonamido substituted 4,5-diaryloxazole were prepared and evaluated for their ability to inhibit the inducible form of cyclooxygenase (COX-2) in vitro and in vivo. Several unique substitution patterns were identified that led to potent and selective inhibitors of COX-2. In general, 2-trifluoromethly-4,5-diaryloxazoles substituted with a methylsulfonyl or sulfonamido group were particularly potent inhibitors. One of the more potent compounds with a selectivity for COX-2 of about 800 fold was 4b (SC-299). SC-299, a highly fluorescent molecule, may be useful for spectroscopic studies on preferential inhibitor binding to COX-2. © 1999 John Wiley & Sons, Inc. Med Res Rev, 19, No. 3, 199–208, 1999. |
| تدمد: | 1098-1128 0198-6325 |
| DOI: | 10.1002/(sici)1098-1128(199905)19:3<199::aid-med1>3.0.co;2-7 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_________::efe6962fa7e482f1968255b75b942a14 https://doi.org/10.1002/(sici)1098-1128(199905)19:3<199::aid-med1>3.0.co;2-7 |
| Rights: | CLOSED |
| رقم الانضمام: | edsair.doi...........efe6962fa7e482f1968255b75b942a14 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 10981128 01986325 |
|---|---|
| DOI: | 10.1002/(sici)1098-1128(199905)19:3<199::aid-med1>3.0.co;2-7 |