Bioorganic & medicinal chemistry letters, 2006-03, Vol.16 (5), p.1202-1206
- Sakya, Subas M.
- Cheng, Hengmiao
- Lundy DeMello, Kristin M.
- Shavnya, Andrei
- Minich, Martha L.
- Rast, Bryson
- Dutra, Jason
- Li, Chao
- Rafka, Robert J.
- Koss, David A.
- Li, Jin
- Jaynes, Burton H.
- Ziegler, Carl B.
- Mann, Donald W.
- Petras, Carol F.
- Seibel, Scott B.
- Silvia, Annette M.
- George, David M.
- Hickman, Anne
- Haven, Michelle L.
- Lynch, Michael P.
2006
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- Autor(en) / Beteiligte
- Sakya, Subas M.
- Cheng, Hengmiao
- Lundy DeMello, Kristin M.
- Shavnya, Andrei
- Minich, Martha L.
- Rast, Bryson
- Dutra, Jason
- Li, Chao
- Rafka, Robert J.
- Koss, David A.
- Li, Jin
- Jaynes, Burton H.
- Ziegler, Carl B.
- Mann, Donald W.
- Petras, Carol F.
- Seibel, Scott B.
- Silvia, Annette M.
- George, David M.
- Hickman, Anne
- Haven, Michelle L.
- Lynch, Michael P.
- Titel
- 5-Heteroatom-substituted pyrazoles as canine COX-2 inhibitors: Part 2. Structure–activity relationship studies of 5-alkylethers and 5-thioethers
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2006-03, Vol.16 (5), p.1202-1206
- Ort / Verlag
- Oxford: Elsevier Ltd
- Erscheinungsjahr
- 2006
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- Structure–activity relationship (SAR) studies of novel 2-[3-trifluoromethyl-5-alkyl(thio)ether pyrazo-1-yl]-5-methanesulfonyl pyridine derivatives for canine COX enzymes are described. The 4-cyano-5-alkyl ethers were found to have excellent potency and selectivity, whereas the 5-thioethers were potent but less selective than the ether analogs in a canine whole blood (CWB) COX-2 assay. Structure–activity relationship (SAR) studies of novel 2-[3-trifluoromethyl-5-alkyl(thio)ether pyrazo-1-yl]-5-methanesulfonyl pyridine derivatives for canine COX enzymes are described. The 4-cyano-5-alkyl ethers were found to have excellent potency and selectivity, whereas the 5-thioethers were potent but less selective than the ether analogs in a canine whole blood (CWB) COX-2 assay.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2005.11.110Titel-ID: cdi_proquest_miscellaneous_19372374
- Format
- –
- Schlagworte
- Aanine, Alkylation, Animals, Biological and medical sciences, Bones, joints and connective tissue. Antiinflammatory agents, COX-1, COX-2, Cyclooxygenase 2 - metabolism, Cyclooxygenase 2 Inhibitors - chemical synthesis, Cyclooxygenase 2 Inhibitors - chemistry, Cyclooxygenase 2 Inhibitors - pharmacokinetics, Cyclooxygenase 2 Inhibitors - pharmacology, Dogs, Ethers - chemistry, Heteroatom, Inhibitory Concentration 50, Medical sciences, Molecular Structure, Pharmacology. Drug treatments, Pyrazoles, Pyrazoles - chemistry, SAR, Structure-Activity Relationship, Sulfhydryl Compounds - chemistry