Identification of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimi-dinyl] amines and ethers as potent and selective cyclooxygenase-2 inhibitors
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| Published in | Bioorganic & medicinal chemistry letters Vol. 19; no. 15; pp. 4504 - 4508 |
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| Main Authors | , , , , , , , , , , , , , , , , , , , , , , , , , , , |
| Format | Journal Article |
| Language | English |
| Published |
Amsterdam
Elsevier
2009
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| Subjects | |
| Online Access | Get full text |
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| Author | KLEANTHOUS, Sawas PAYNE, Jeremy J LAMBETH, Paul F LUCAS, Fiona S SWARBRICK, Martin E STEVENS, Alexander J BESWICK, Paul J WISEMAN, Joanne O GREEN, Richard H STOCKER, Richard PAGE, Lee W MATHEWS, Neil CORFIELD, John A BOUNTRA, Chas GLEAVE, Robert J NAYLOR, Alan COLLINS, Sue D CARTER, Malcolm C HARTLEY, C. David PEGG, Neil A STUART, Alastair J CLAYTON, Nick M SKIDMORE, John PRICE, Helen S CHESSELL, Lain P STRATTON, Sharon C BINGHAM, Sharon CHAMBERS, Laura J |
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| Author_xml | – sequence: 1 givenname: Martin E surname: SWARBRICK fullname: SWARBRICK, Martin E organization: Pain and Neuroexcitability Discovery Performance Unit, Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom – sequence: 2 givenname: Paul J surname: BESWICK fullname: BESWICK, Paul J organization: Pain and Neuroexcitability Discovery Performance Unit, Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom – sequence: 3 givenname: Sue D surname: COLLINS fullname: COLLINS, Sue D organization: Pain and Neuroexcitability Discovery Performance Unit, Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom – sequence: 4 givenname: John A surname: CORFIELD fullname: CORFIELD, John A organization: Pain and Neuroexcitability Discovery Performance Unit, Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom – sequence: 5 givenname: C. David surname: HARTLEY fullname: HARTLEY, C. David organization: Pain and Neuroexcitability Discovery Performance Unit, Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom – sequence: 6 givenname: Sawas surname: KLEANTHOUS fullname: KLEANTHOUS, Sawas organization: Pain and Neuroexcitability Discovery Performance Unit, Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom – sequence: 7 givenname: Paul F surname: LAMBETH fullname: LAMBETH, Paul F organization: Pain and Neuroexcitability Discovery Performance Unit, Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom – sequence: 8 givenname: Fiona S surname: LUCAS fullname: LUCAS, Fiona S organization: Pain and Neuroexcitability Discovery Performance Unit, Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom – sequence: 9 givenname: Neil surname: MATHEWS fullname: MATHEWS, Neil organization: Pain and Neuroexcitability Discovery Performance Unit, Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom – sequence: 10 givenname: Alan surname: NAYLOR fullname: NAYLOR, Alan organization: Pain and Neuroexcitability Discovery Performance Unit, Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom – sequence: 11 givenname: Lee W surname: PAGE fullname: PAGE, Lee W organization: Pain and Neuroexcitability Discovery Performance Unit, Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom – sequence: 12 givenname: Jeremy J surname: PAYNE fullname: PAYNE, Jeremy J organization: Pain and Neuroexcitability Discovery Performance Unit, Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom – sequence: 13 givenname: Robert J surname: GLEAVE fullname: GLEAVE, Robert J organization: Pain and Neuroexcitability Discovery Performance Unit, Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom – sequence: 14 givenname: Neil A surname: PEGG fullname: PEGG, Neil A organization: Pain and Neuroexcitability Discovery Performance Unit, Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom – sequence: 15 givenname: Helen S surname: PRICE fullname: PRICE, Helen S organization: Pain and Neuroexcitability Discovery Performance Unit, Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom – sequence: 16 givenname: John surname: SKIDMORE fullname: SKIDMORE, John organization: Pain and Neuroexcitability Discovery Performance Unit, Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom – sequence: 17 givenname: Alexander J surname: STEVENS fullname: STEVENS, Alexander J organization: Pain and Neuroexcitability Discovery Performance Unit, Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom – sequence: 18 givenname: Richard surname: STOCKER fullname: STOCKER, Richard organization: Pain and Neuroexcitability Discovery Performance Unit, Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom – sequence: 19 givenname: Sharon C surname: STRATTON fullname: STRATTON, Sharon C organization: Pain and Neuroexcitability Discovery Performance Unit, Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom – sequence: 20 givenname: Alastair J surname: STUART fullname: STUART, Alastair J organization: Pain and Neuroexcitability Discovery Performance Unit, Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom – sequence: 21 givenname: Joanne O surname: WISEMAN fullname: WISEMAN, Joanne O organization: Pain and Neuroexcitability Discovery Performance Unit, Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom – sequence: 22 givenname: Richard H surname: GREEN fullname: GREEN, Richard H organization: Pain and Neuroexcitability Discovery Performance Unit, Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom – sequence: 23 givenname: Sharon surname: BINGHAM fullname: BINGHAM, Sharon organization: Pain and Neuroexcitability Discovery Performance Unit, Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom – sequence: 24 givenname: Chas surname: BOUNTRA fullname: BOUNTRA, Chas organization: Pain and Neuroexcitability Discovery Performance Unit, Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom – sequence: 25 givenname: Malcolm C surname: CARTER fullname: CARTER, Malcolm C organization: Pain and Neuroexcitability Discovery Performance Unit, Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom – sequence: 26 givenname: Laura J surname: CHAMBERS fullname: CHAMBERS, Laura J organization: Pain and Neuroexcitability Discovery Performance Unit, Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom – sequence: 27 givenname: Lain P surname: CHESSELL fullname: CHESSELL, Lain P organization: Pain and Neuroexcitability Discovery Performance Unit, Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom – sequence: 28 givenname: Nick M surname: CLAYTON fullname: CLAYTON, Nick M organization: Pain and Neuroexcitability Discovery Performance Unit, Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom |
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| Keywords | CNS penetrant Prostaglandin-endoperoxide synthase Intravenous administration Rat Sulfone COX-2 Nitrogen heterocycle Cyclooxygenase 2 Cyclooxygenase 2 inhibitor Selectivity Blood brain barrier Pyrimidine Cyclooxygenase Structure activity relation Six membered ring Chemical synthesis Enzyme Rodentia Benzene derivatives Oral administration Enzyme inhibitor Bioavailability In vitro Non steroidal antiinflammatory agent In vivo Vertebrata Mammalia Animal Fluorine Organic compounds Oxidoreductases Pharmacokinetics |
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| SubjectTerms | Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Medical sciences Pharmacology. Drug treatments |
| Title | Identification of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimi-dinyl] amines and ethers as potent and selective cyclooxygenase-2 inhibitors |
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