-
1
-
-
0034527045
-
The fight against rheumatism: From willow bark to COX-1 sparing drugs
-
Vane, J. R. The fight against rheumatism: From willow bark to COX-1 sparing drugs. J. Physiol. Pharmacol. 2000, 51, 573-586.
-
(2000)
J. Physiol. Pharmacol
, vol.51
, pp. 573-586
-
-
Vane, J.R.1
-
2
-
-
65249118795
-
The COXIB experience: A look in the rearview mirror
-
Marnett, L. J. The COXIB experience: A look in the rearview mirror. Annu. Rev. Pharmacol. Toxicol. 2009, 49, 265-290.
-
(2009)
Annu. Rev. Pharmacol. Toxicol
, vol.49
, pp. 265-290
-
-
Marnett, L.J.1
-
3
-
-
76149143424
-
Trends in the non-steroidal anti-inflammatory drug market in six central-eastern european countries based on retail information
-
Inotai, A.; Hanko, B.; Meszaro, A. Trends in the non-steroidal anti-inflammatory drug market in six central-eastern european countries based on retail information. Pharmacoepidemiol. Drug Saf. 2010, 19, 183-190.
-
(2010)
Pharmacoepidemiol. Drug Saf
, vol.19
, pp. 183-190
-
-
Inotai, A.1
Hanko, B.2
Meszaro, A.3
-
4
-
-
0027480087
-
Differential inhibition of prostaglandin endoperoxide synthase (cyclooxygenase) isozymes by aspirin and other non-steroidal anti-inflammatory drugs
-
Meade, E. A.; Smith, W. L.; DeWitt, D. L. Differential inhibition of prostaglandin endoperoxide synthase (cyclooxygenase) isozymes by aspirin and other non-steroidal anti-inflammatory drugs. J. Biol. Chem. 1993, 268, 6610-6614.
-
(1993)
J. Biol. Chem
, vol.268
, pp. 6610-6614
-
-
Meade, E.A.1
Smith, W.L.2
Dewitt, D.L.3
-
5
-
-
0033288941
-
Selective inhibitors of cyclooxygenase-2 (COX-2)
-
Talley, J. J. Selective inhibitors of cyclooxygenase-2 (COX-2). Prog. Med. Chem. Res. 1999, 36, 201-234.
-
(1999)
Prog. Med. Chem. Res
, vol.36
, pp. 201-234
-
-
Talley, J.J.1
-
6
-
-
23244467981
-
Selective cycloxygenase-2 inhibitors
-
Black, W. C. Selective cycloxygenase-2 inhibitors. Annu. Rep. Med. Chem. 2004, 39, 125-138.
-
(2004)
Annu. Rep. Med. Chem
, vol.39
, pp. 125-138
-
-
Black, W.C.1
-
7
-
-
13444266910
-
Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: Identification of 4-[5-(4- methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide (SC-58635, celecoxib)
-
Penning, T. D.; Talley, J. J.; Bertenshaw, S.R.; Carter, J. S.; Collins, P. W.; Docter, S.; Graneto, M. J.; Lee, L. F.; Malecha, J. W.; Miyashiro, J. M.; Rogers, R. S.; Rogier, D. J.; Yu, S. S.; Anderson, G. D.; Burton, E. G.; Cogburn, J. N.; Gregory, S. A.; Koboldt, C. M.; Perkins, W. E.; Seibert, K.; Veenhuizen, A. W.; Zhang, Y. Y.; Isakson, P. C. Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4- methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide (SC-58635, celecoxib). J. Med. Chem. 1997, 40, 1347-1365.
-
(1997)
J. Med. Chem
, vol.40
, pp. 1347-1365
-
-
Penning, T.D.1
Talley, J.J.2
Bertenshaw, S.R.3
Carter, J.S.4
Collins, P.W.5
Docter, S.6
Graneto, M.J.7
Lee, L.F.8
Malecha, J.W.9
Miyashiro, J.M.10
Rogers, R.S.11
Rogier, D.J.12
Yu, S.S.13
Anderson, G.D.14
Burton, E.G.15
Cogburn, J.N.16
Gregory, S.A.17
Koboldt, C.M.18
Perkins, W.E.19
Seibert, K.20
Veenhuizen, A.W.21
Zhang, Y.Y.22
Isakson, P.C.23
more..
-
8
-
-
0033526928
-
The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2- inhibitor
-
Prasit, P.; Wang, Z.; Brideau, C.; Chan, C. C.; Charleson, S.; Cromlish, W.; Ethier, D.; Evans, J. F.; Ford-Hutchinson, A. W.; Gauthier, J. Y.; Gordon, R.; Guay, J.; Gresser, M.; Kargman, S.; Kennedy, B.; Leblanc, Y.; Léger, S.; Mancini, J.; O'Neill, G. P.; Ouellet, M.; Percival, M. D.; Perrier, H.; Riendeau, D.; Rodger, I.; Zamboni, R. The discovery of rofecoxib, [MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone], an orally active cyclooxygenase-2- inhibitor. Bioorg. Med. Chem. Lett. 1999, 9, 1773-1778.
-
(1999)
Bioorg. Med. Chem. Lett
, vol.9
, pp. 1773-1778
-
-
Prasit, P.1
Wang, Z.2
Brideau, C.3
Chan, C.C.4
Charleson, S.5
Cromlish, W.6
Ethier, D.7
Evans, J.F.8
Ford-Hutchinson, A.W.9
Gauthier, J.Y.10
Gordon, R.11
Guay, J.12
Gresser, M.13
Kargman, S.14
Kennedy, B.15
Leblanc, Y.16
Léger, S.17
Mancini, J.18
O'Neill, G.P.19
Ouellet, M.20
Percival, M.D.21
Perrier, H.22
Riendeau, D.23
Rodger, I.24
Zamboni, R.25
more..
-
9
-
-
0029911267
-
Flexibility of the NSAID binding site in the structure of human cyclooxygenase-2
-
Luong, C.; Miller, A.; Barnett, J.; Chow, J.; Ramesha, C.; Browner, M. F. Flexibility of the NSAID binding site in the structure of human cyclooxygenase-2. Nat. Struct. Biol. 1996, 3, 927-933.
-
(1996)
Nat. Struct. Biol
, vol.3
, pp. 927-933
-
-
Luong, C.1
Miller, A.2
Barnett, J.3
Chow, J.4
Ramesha, C.5
Browner, M.F.6
-
10
-
-
0030461132
-
Structural basis for selective inhibition of cyclooxygenase-2 by anti-inflammatory agents
-
Kurumbail, R. G.; Stevens, A. M.; Gierse, J. K.; McDonald, J. J.; Stegeman, R. A.; Pak, J. Y.; Gildehaus, D.; Miyashiro, J. M.; Penning, T. D.; Seibert, K.; Isakson, P. C.; Stallings, W. C. Structural basis for selective inhibition of cyclooxygenase-2 by anti-inflammatory agents. Nature 1996, 384, 644-648.
-
(1996)
Nature
, vol.384
, pp. 644-648
-
-
Kurumbail, R.G.1
Stevens, A.M.2
Gierse, J.K.3
McDonald, J.J.4
Stegeman, R.A.5
Pak, J.Y.6
Gildehaus, D.7
Miyashiro, J.M.8
Penning, T.D.9
Seibert, K.10
Isakson, P.C.11
Stallings, W.C.12
-
11
-
-
33644870565
-
COX isoforms in the cardiovascular system: Understanding the activities of non-steroidal anti-inflammatory drugs
-
Mitchell, J. A.; Warner, T. D. COX isoforms in the cardiovascular system: Understanding the activities of non-steroidal anti-inflammatory drugs. Nat. Rev. Drug Discov. 2006, 5, 75-85.
-
(2006)
Nat. Rev. Drug Discov
, vol.5
, pp. 75-85
-
-
Mitchell, J.A.1
Warner, T.D.2
-
12
-
-
33749337137
-
Adverse effects of cyclooxygenase 2 inhibitors on renal and arrhythmia events-meta-analysis of randomized trials
-
Zhang, J. J.; Ding, E. L.; Song, Y. Q. Adverse effects of cyclooxygenase 2 inhibitors on renal and arrhythmia events-meta-analysis of randomized trials. JAMA 2006, 296, 1619-1632.
-
(2006)
JAMA
, vol.296
, pp. 1619-1632
-
-
Zhang, J.J.1
Ding, E.L.2
Song, Y.Q.3
-
13
-
-
0031717446
-
Cyclooxygenases as the principle target for the action of NSAIDs
-
Smith, T. J. Cyclooxygenases as the principle target for the action of NSAIDs. Rheum. Clinics N. Amer. 1998, 24, 501-523.
-
(1998)
Rheum. Clinics N. Amer
, vol.24
, pp. 501-523
-
-
Smith, T.J.1
-
14
-
-
70449341873
-
Modulation of inflammatory disease by inhibitors of leukotriene A4 hydrolase
-
Fourie, A. M. Modulation of inflammatory disease by inhibitors of leukotriene A4 hydrolase. Curr. Opin. Investig. Drugs 2009, 10, 1173-1182.
-
(2009)
Curr. Opin. Investig. Drugs
, vol.10
, pp. 1173-1182
-
-
Fourie, A.M.1
-
15
-
-
0042574211
-
Dual inhibition of cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5- LOX) as a new strategy to provide safer nonsteroidal anti-inflammatory drugs
-
Charlier, C.; Michaux, C. Dual inhibition of cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5- LOX) as a new strategy to provide safer nonsteroidal anti-inflammatory drugs. Eur. J. Med. Chem. 2003, 38, 645-659.
-
(2003)
Eur. J. Med. Chem
, vol.38
, pp. 645-659
-
-
Charlier, C.1
Michaux, C.2
-
16
-
-
77949363808
-
The 5-lipoxygenase/leukotriene pathway in preclinical models of cardiovascular disease
-
Poeckel, D.; Funk, C. D. The 5-lipoxygenase/leukotriene pathway in preclinical models of cardiovascular disease. Cardiovasc. Res. 2010, 86, 243-253.
-
(2010)
Cardiovasc. Res
, vol.86
, pp. 243-253
-
-
Poeckel, D.1
Funk, C.D.2
-
17
-
-
29244449354
-
Prostaglandins and cancer
-
Wang, D.; Dubois, R. N. Prostaglandins and cancer. Gut 2006, 55, 115-122.
-
(2006)
Gut
, vol.55
, pp. 115-122
-
-
Wang, D.1
Dubois, R.N.2
-
18
-
-
34047105383
-
NSAIDs and cancer prevention: Targets downstream of COX-2
-
Cha, Y. I.; Dubois, R. N. NSAIDs and cancer prevention: targets downstream of COX-2. Annu. Rev. Med. 2007, 58, 239-252.
-
(2007)
Annu. Rev. Med
, vol.58
, pp. 239-252
-
-
Cha, Y.I.1
Dubois, R.N.2
-
19
-
-
0142058174
-
Anti-TNF-therapies: The next generation
-
Palladino, M. A.; Bahjat, F. R.; Theodorakis, E. A.; Moldaver, L. L. Anti-TNF-therapies: The next generation. Nat. Rev. Drug Disc. 2003, 2, 736-746.
-
(2003)
Nat. Rev. Drug Disc
, vol.2
, pp. 736-746
-
-
Palladino, M.A.1
Bahjat, F.R.2
Theodorakis, E.A.3
Moldaver, L.L.4
-
20
-
-
54949101585
-
Cytokines and their relationship to the symptoms and outcome of cancer
-
Seruga, B.; Zhang, H.; Bernstein, L. J.; Tannock, I. F. Cytokines and their relationship to the symptoms and outcome of cancer. Nat. Rev. Cancer 2008, 8, 887-899.
-
(2008)
Nat. Rev. Cancer
, vol.8
, pp. 887-899
-
-
Seruga, B.1
Zhang, H.2
Bernstein, L.J.3
Tannock, I.F.4
-
21
-
-
27144475571
-
Neuroinflammation: A potential therapeutic target
-
Craft, J. M.; Watterson, D. M.; Van Eldik, L. J. Neuroinflammation: A potential therapeutic target. Expert Opin. Ther. Targets 2005, 9, 887-900.
-
(2005)
Expert Opin. Ther. Targets
, vol.9
, pp. 887-900
-
-
Craft, J.M.1
Watterson, D.M.2
van Eldik, L.J.3
-
22
-
-
74549220751
-
COX-2 inhibitors as antidepressants and antipsychotics: Clinical evidence
-
Muller, N. COX-2 inhibitors as antidepressants and antipsychotics: Clinical evidence. Curr. Opin. Invest. Drugs 2010, 11, 31-42.
-
(2010)
Curr. Opin. Invest. Drugs
, vol.11
, pp. 31-42
-
-
Muller, N.1
-
23
-
-
34547598278
-
Anti-inflammatory drugs in the 21st century
-
Rainsford, K. D. Anti-inflammatory drugs in the 21st century. Subcell. Biochem. 2007, 42, 3-27.
-
(2007)
Subcell. Biochem
, vol.42
, pp. 3-27
-
-
Rainsford, K.D.1
-
24
-
-
0036562261
-
Potential cardioprotective actions of NO-releasing aspirin
-
Wallace, J. L.; Ignarro, L. J.; Fiorucci, S. Potential cardioprotective actions of NO-releasing aspirin. Nat. Rev. Drug Discov. 2002, 1, 375-382.
-
(2002)
Nat. Rev. Drug Discov
, vol.1
, pp. 375-382
-
-
Wallace, J.L.1
Ignarro, L.J.2
Fiorucci, S.3
-
25
-
-
0031776628
-
Chemistry and structure-activity relationships of leukotriene receptor antagonists
-
Bernstein, P. Chemistry and structure-activity relationships of leukotriene receptor antagonists. Am. J. Respir. Crit. Care Med. 1998, 157, S220-S226.
-
(1998)
Am. J. Respir. Crit. Care Med
, vol.157
-
-
Bernstein, P.1
-
26
-
-
12944265473
-
Nitric oxide prevents cardiovascular disease and determines survival in polyglobulic mice overexpressing erythropoietin
-
Ruschitzka, F. T.; Wenger, R. H.; Stallmach, T.; Quaschning, T.; de Wit, C.; Wagner, K.; Labugger, R.; Kelm, M.; Noll, G.; Rülicke, T.; Shaw, S.; Lindberg, R. L.; Rodenwaldt, B.; Lutz, H.; Bauer, C.; Lüscher, T. F.; Gassmann, M. Nitric oxide prevents cardiovascular disease and determines survival in polyglobulic mice overexpressing erythropoietin. Proc. Natl. Acad. Sci. USA 2000, 97, 11609-11613.
-
(2000)
Proc. Natl. Acad. Sci. USA
, vol.97
, pp. 11609-11613
-
-
Ruschitzka, F.T.1
Wenger, R.H.2
Stallmach, T.3
Quaschning, T.4
de Wit, C.5
Wagner, K.6
Labugger, R.7
Kelm, M.8
Noll, G.9
Rülicke, T.10
Shaw, S.11
Lindberg, R.L.12
Rodenwaldt, B.13
Lutz, H.14
Bauer, C.15
Lüscher, T.F.16
Gassmann, M.17
-
27
-
-
0008915459
-
Effects of a nitric oxide-releasing naproxen derivative on hypertension and gastric damage induced by chronic nitric oxide inhibition in the rat
-
Muscara, M. N.; McNight, W.; Del Soldato, P.; Wallace, J. L. Effects of a nitric oxide-releasing naproxen derivative on hypertension and gastric damage induced by chronic nitric oxide inhibition in the rat. Pharmacol. Lett. 1998, 62, 235-240.
-
(1998)
Pharmacol. Lett
, vol.62
, pp. 235-240
-
-
Muscara, M.N.1
McNight, W.2
del Soldato, P.3
Wallace, J.L.4
-
28
-
-
0034687219
-
Nitrosothiol esters of diclofenac: Synthesis and pharmacological characterization as gastrointestinal-sparing prodrugs
-
Bandarage, U. K.; Chen, L.; Fang, X.; Garvey, D. S.; Glavin, A.; Janero, D. R.; Letts, L. G.; Mercer, G. J.; Saha, J. K.; Schroeder, J. D.; Shumway, M. J.; Tam, S. W. Nitrosothiol esters of diclofenac: Synthesis and pharmacological characterization as gastrointestinal-sparing prodrugs. J. Med. Chem. 2000, 43, 4005-4016.
-
(2000)
J. Med. Chem
, vol.43
, pp. 4005-4016
-
-
Bandarage, U.K.1
Chen, L.2
Fang, X.3
Garvey, D.S.4
Glavin, A.5
Janero, D.R.6
Letts, L.G.7
Mercer, G.J.8
Saha, J.K.9
Schroeder, J.D.10
Shumway, M.J.11
Tam, S.W.12
-
29
-
-
0034656841
-
Diazeniumdiolates: Pro- and antioxidant applications of the NONOates
-
Fitzhugh, A. L.; Keefer, L. K. Diazeniumdiolates: pro- and antioxidant applications of the NONOates. Free Radic. Biol. Med. 2000, 28, 1463-1469.
-
(2000)
Free Radic. Biol. Med
, vol.28
, pp. 1463-1469
-
-
Fitzhugh, A.L.1
Keefer, L.K.2
-
30
-
-
20444373321
-
Novel nonsteroidal anti-inflammatory drugs possessing a nitric oxide donor diazen-1-ium-1,2-diolate moiety: Design, synthesis, biological evaluation, and nitric oxide release studies
-
Velázquez, C. A.; Rao, P. N. P.; Knaus, E. E. Novel nonsteroidal anti-inflammatory drugs possessing a nitric oxide donor diazen-1-ium-1,2-diolate moiety: design, synthesis, biological evaluation, and nitric oxide release studies. J. Med. Chem. 2005, 48, 4061-4067.
-
(2005)
J. Med. Chem
, vol.48
, pp. 4061-4067
-
-
Velázquez, C.A.1
Rao, P.N.P.2
Knaus, E.E.3
-
31
-
-
41149109145
-
Second-generation aspirin and indomethacin prodrugs possessing an O2-(acetoxymethyl)-1-(2-carboxypyrrolidin-1- yl)diazenium-1,2-diolate nitric oxide donor moiety: Design, synthesis, biological evaluation, and nitric oxide release studies
-
Velázquez, C. A.; Chen, Q. H.; Citro, M. L.; Keefer, L. K.; Knaus, E. E. Second-generation aspirin and indomethacin prodrugs possessing an O2-(acetoxymethyl)-1-(2-carboxypyrrolidin-1- yl)diazenium-1,2-diolate nitric oxide donor moiety: Design, synthesis, biological evaluation, and nitric oxide release studies. J. Med. Chem. 2008, 51, 1954-1961.
-
(2008)
J. Med. Chem
, vol.51
, pp. 1954-1961
-
-
Velázquez, C.A.1
Chen, Q.H.2
Citro, M.L.3
Keefer, L.K.4
Knaus, E.E.5
-
32
-
-
34147113829
-
NO-donor COX-2 inhibitors: New nitrooxy-substituted 1,5-diarylimidazoles endowed with COX-2 inhibitory and vasodilator properties
-
Chegaev, K.; Lazzarato, L.; Tosco, P.; Cena, C.; Marini, E.; Rolando, B.; Carrupt, P. A.; Fruttero, R.; Gasco, A. NO-donor COX-2 inhibitors: New nitrooxy-substituted 1,5-diarylimidazoles endowed with COX-2 inhibitory and vasodilator properties. J. Med. Chem. 2007, 50, 1449-1457.
-
(2007)
J. Med. Chem
, vol.50
, pp. 1449-1457
-
-
Chegaev, K.1
Lazzarato, L.2
Tosco, P.3
Cena, C.4
Marini, E.5
Rolando, B.6
Carrupt, P.A.7
Fruttero, R.8
Gasco, A.9
-
33
-
-
37048998977
-
Structure-based design, synthesis, and biological evaluation of indomethacin derivatives as cyclooxygenase-2 inhibiting nitric oxide donors
-
Wey, S. J.; Augustyniak, M. E.; Cochran, E. D.; Ellis, J. L.; Fang, X.; Garvey, D. S.; Janero, D. R.; Letts, L. G.; Martino, A. M.; Melim, T. L.; Murty, M. G.; Richardson, S. K.; Schroeder, J. D.; Selig, W. M.; Trocha, A. M.; Wexler, R. S.; Young, D. V., Zemtseva, I. S.; Zifcak, B. M. Structure-based design, synthesis, and biological evaluation of indomethacin derivatives as cyclooxygenase-2 inhibiting nitric oxide donors. J. Med. Chem. 2007, 50, 6367-6382.
-
(2007)
J. Med. Chem
, vol.50
, pp. 6367-6382
-
-
Wey, S.J.1
Augustyniak, M.E.2
Cochran, E.D.3
Ellis, J.L.4
Fang, X.5
Garvey, D.S.6
Janero, D.R.7
Letts, L.G.8
Martino, A.M.9
Melim, T.L.10
Murty, M.G.11
Richardson, S.K.12
Schroeder, J.D.13
Selig, W.M.14
Trocha, A.M.15
Wexler, R.S.16
Young, D.V.17
Zemtseva, I.S.18
Zifcak, B.M.19
-
34
-
-
41149115687
-
Searching for new NO-donor aspirin-like molecules: A new class of nitrooxy-acyl derivatives of salicylic acid
-
Lazzarato, L.; Donnola, M.; Rolando, B.; Marini, E.; Cena, C.; Coruzzi, G.; Guaita, E.; Morini, G.; Fruttero, R.; Gasco, A.; Biondi, S. Searching for new NO-donor aspirin-like molecules: A new class of nitrooxy-acyl derivatives of salicylic acid. J. Med. Chem. 2008, 51, 1894-1903.
-
(2008)
J. Med. Chem
, vol.51
, pp. 1894-1903
-
-
Lazzarato, L.1
Donnola, M.2
Rolando, B.3
Marini, E.4
Cena, C.5
Coruzzi, G.6
Guaita, E.7
Morini, G.8
Fruttero, R.9
Gasco, A.10
Biondi, S.11
-
35
-
-
58149104269
-
Discovery of a true aspirin prodrug
-
Moriarty, L. M.; Lally, M. N.; Carolan, C. G.; Jones, M.; Clancy, J. M.; Gilmer, J. F. Discovery of a true aspirin prodrug. J. Med. Chem. 2008, 51, 7991-7999.
-
(2008)
J. Med. Chem
, vol.51
, pp. 7991-7999
-
-
Moriarty, L.M.1
Lally, M.N.2
Carolan, C.G.3
Jones, M.4
Clancy, J.M.5
Gilmer, J.F.6
-
36
-
-
69049098127
-
Nitrooxyacyloxy methyl esters of aspirin as novel nitric oxide releasing aspirins
-
Lazzarato, L.; Donnola, M.; Rolando, B.; Chegaev, K.; Marini, E.; Cena, C.; Di Stilo, A.; Fruttero, R.; Biondi, S.; Ongini, E.; Gasco, A. (Nitrooxyacyloxy)methyl esters of aspirin as novel nitric oxide releasing aspirins. J. Med. Chem. 2009, 52, 5058-5068.
-
(2009)
J. Med. Chem
, vol.52
, pp. 5058-5068
-
-
Lazzarato, L.1
Donnola, M.2
Rolando, B.3
Chegaev, K.4
Marini, E.5
Cena, C.6
Di Stilo, A.7
Fruttero, R.8
Biondi, S.9
Ongini, E.10
Gasco, A.11
-
37
-
-
70350257912
-
Apricoxib, a COX-2 inhibitor for the potential treatment of pain and cancer
-
Rao, P. N. P.; Rajesh, K. G. Apricoxib, a COX-2 inhibitor for the potential treatment of pain and cancer. IDrugs 2009, 12, 711-722.
-
(2009)
IDrugs
, vol.12
, pp. 711-722
-
-
Rao, P.N.P.1
Rajesh, K.G.2
-
38
-
-
35948946191
-
Cyclooxygenase-2 inhibitors. 1,5-diarylpyrrol-3-acetic esters with enhanced inhibitory activity toward cyclooxygenase-2 and improved cyclooxygenase-2/cyclooxygenase-1 selectivity
-
Biava, M.; Porretta, G. C.; Poce, G.; Supino, S.; Forli, S.; Rovini, M.; Cappelli, A.; Manetti, F.; Botta, M.; Sautebin, L.; Rossi, A.; Pergola, C.; Ghelardini, C.; Vivoli, E.; Makovec, F.; Anzellotti, P.; Patrignani, P.; Anzini, M. Cyclooxygenase-2 inhibitors. 1,5-diarylpyrrol-3-acetic esters with enhanced inhibitory activity toward cyclooxygenase-2 and improved cyclooxygenase-2/cyclooxygenase-1 selectivity. J. Med. Chem. 2007, 50, 5403-5411.
-
(2007)
J. Med. Chem
, vol.50
, pp. 5403-5411
-
-
Biava, M.1
Porretta, G.C.2
Poce, G.3
Supino, S.4
Forli, S.5
Rovini, M.6
Cappelli, A.7
Manetti, F.8
Botta, M.9
Sautebin, L.10
Rossi, A.11
Pergola, C.12
Ghelardini, C.13
Vivoli, E.14
Makovec, F.15
Anzellotti, P.16
Patrignani, P.17
Anzini, M.18
-
39
-
-
49449083101
-
Synthesis, biological evaluation, and enzyme docking simulations of 1,5-diarylpyrrole 3-alkoxyethyl ethers as selective cyclooxygenase-2 inhibitors endowed with anti-inflammatory and antinociceptive activity
-
Anzini, M.; Rovini, M.; Cappelli, A.; Vomero, S.; Manetti, F.; Botta, M.; Sautebin, L.; Rossi, A.; Pergola, C.; Ghelardini, C.; Norcini, M.; Giordani, A.; Makovec, F.; Anzellotti, P.; Patrignani, P.; Biava, M. Synthesis, biological evaluation, and enzyme docking simulations of 1,5-diarylpyrrole 3-alkoxyethyl ethers as selective cyclooxygenase-2 inhibitors endowed with anti-inflammatory and antinociceptive activity. J. Med. Chem. 2008, 51, 4476-4481.
-
(2008)
J. Med. Chem
, vol.51
, pp. 4476-4481
-
-
Anzini, M.1
Rovini, M.2
Cappelli, A.3
Vomero, S.4
Manetti, F.5
Botta, M.6
Sautebin, L.7
Rossi, A.8
Pergola, C.9
Ghelardini, C.10
Norcini, M.11
Giordani, A.12
Makovec, F.13
Anzellotti, P.14
Patrignani, P.15
Biava, M.16
-
40
-
-
77249138784
-
Novel ester and acid derivatives of the 1,5-diarylpyrrole scaffold as anti-inflammatory and analgesic agents: Synthesis and in vitro and in vivo biological evaluation
-
Biava, M.; Porretta, G. C.; Poce, G.; Battilocchio, C.; Manetti, F.; Botta, M.; Forli, S.; Sautebin, L.; Rossi, A.; Pergola, C.; Ghelardini, C.; Galeotti, N.; Makovec, F.; Giordani, A.; Anzellotti, P.; Patrignani, P.; Anzini, M. Novel ester and acid derivatives of the 1,5-diarylpyrrole scaffold as anti-inflammatory and analgesic agents: Synthesis and in vitro and in vivo biological evaluation. J. Med. Chem. 2010, 53, 723-733.
-
(2010)
J. Med. Chem
, vol.53
, pp. 723-733
-
-
Biava, M.1
Porretta, G.C.2
Poce, G.3
Battilocchio, C.4
Manetti, F.5
Botta, M.6
Forli, S.7
Sautebin, L.8
Rossi, A.9
Pergola, C.10
Ghelardini, C.11
Galeotti, N.12
Makovec, F.13
Giordani, A.14
Anzellotti, P.15
Patrignani, P.16
Anzini, M.17
-
41
-
-
44249120031
-
Evaluation of COX-1/COX-2 selectivity and potency of a new class of COX-2 inhibitors
-
Gierse, J.; Nickols, M.; Leahy, K.; Warner, J.; Zhang, Y.; Cortes-Burgos, L.; Carter, J.; Seibert, K.; Masferrer, J. Evaluation of COX-1/COX-2 selectivity and potency of a new class of COX-2 inhibitors. Eur. J. Pharmacol. 2008, 588, 93-98.
-
(2008)
Eur. J. Pharmacol
, vol.588
, pp. 93-98
-
-
Gierse, J.1
Nickols, M.2
Leahy, K.3
Warner, J.4
Zhang, Y.5
Cortes-Burgos, L.6
Carter, J.7
Seibert, K.8
Masferrer, J.9
-
42
-
-
70349641040
-
Pyridine analogues of nimesulide: Design, synthesis, and in vitro and in vivo pharmacological evaluation as promising cyclooxygenase 1 and 2 inhibitors
-
Renard, J. F.; Arslan, D.; Garbacki, N.; Pirotte, B.; de Leval, X. Pyridine analogues of nimesulide: design, synthesis, and in vitro and in vivo pharmacological evaluation as promising cyclooxygenase 1 and 2 inhibitors. J. Med. Chem. 2009, 52, 5864-5871.
-
(2009)
J. Med. Chem
, vol.52
, pp. 5864-5871
-
-
Renard, J.F.1
Arslan, D.2
Garbacki, N.3
Pirotte, B.4
de Leval, X.5
-
43
-
-
67649968894
-
Identification of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidinyl] amines and ethers as potent and selective cyclooxygenase-2 inhibitors
-
Swarbrick, M. E.; Beswick, P. J.; Gleave, R. J.; Green, R. H.; Bingham, S.; Bountra, C.; Carter, M. C.; Chambers, L. J.; Chessell, I. P.; Clayton, N. M.; Collins, S. D.; Corfield, J. A.; Hartley, C. D.; Kleanthous, S.; Lambeth, P. F.; Lucas, F. S.; Mathews, N.; Naylor, A.; Page, L. W.; Payne, J. J.; Pegg, N. A.; Price, H. S.; Skidmore, J.; Stevens, A. J.; Stocker, R.; Stratton, S. C.; Stuart, A. J.; Wiseman, J. O. Identification of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidinyl] amines and ethers as potent and selective cyclooxygenase-2 inhibitors. Bioorg. Med. Chem. Lett. 2009, 19, 4504-4508.
-
(2009)
Bioorg. Med. Chem. Lett
, vol.19
, pp. 4504-4508
-
-
Swarbrick, M.E.1
Beswick, P.J.2
Gleave, R.J.3
Green, R.H.4
Bingham, S.5
Bountra, C.6
Carter, M.C.7
Chambers, L.J.8
Chessell, I.P.9
Clayton, N.M.10
Collins, S.D.11
Corfield, J.A.12
Hartley, C.D.13
Kleanthous, S.14
Lambeth, P.F.15
Lucas, F.S.16
Mathews, N.17
Naylor, A.18
Page, L.W.19
Payne, J.J.20
Pegg, N.A.21
Price, H.S.22
Skidmore, J.23
Stevens, A.J.24
Stocker, R.25
Stratton, S.C.26
Stuart, A.J.27
Wiseman, J.O.28
more..
-
44
-
-
67650045869
-
Identification and optimisation of a novel series of pyrimidine based cyclooxygenase-2 (COX-2) inhibitors. Utilisation of a biotransformation approach
-
Beswick, P. J.; Blackaby, A. P.; Bountra, C.; Brown, T.; Browning, K.; Campbell, I. B.; Corfield, J.; Gleave, R. J.; Guntrip, S. B.; Hall, R. M.; Hindley, S.; Lambeth, P. F.; Lucas, F.; Mathews, N.; Naylor, A.; Player, H.; Price, H. S.; Sidebottom, P. J.; Taylor, N. L.; Webb, G.; Wiseman, J. Identification and optimisation of a novel series of pyrimidine based cyclooxygenase-2 (COX-2) inhibitors. Utilisation of a biotransformation approach. Bioorg. Med. Chem. Lett. 2009, 19, 4509-4514.
-
(2009)
Bioorg. Med. Chem. Lett
, vol.19
, pp. 4509-4514
-
-
Beswick, P.J.1
Blackaby, A.P.2
Bountra, C.3
Brown, T.4
Browning, K.5
Campbell, I.B.6
Corfield, J.7
Gleave, R.J.8
Guntrip, S.B.9
Hall, R.M.10
Hindley, S.11
Lambeth, P.F.12
Lucas, F.13
Mathews, N.14
Naylor, A.15
Player, H.16
Price, H.S.17
Sidebottom, P.J.18
Taylor, N.L.19
Webb, G.20
Wiseman, J.21
more..
-
45
-
-
69949150537
-
The search for new COX-2 inhibitors: A review of 2002-2008 patents
-
Ramalho, T. C.; Rocha, M. V. J.; Da Cunna, E. F. F.; Freitas, M. P. The search for new COX-2 inhibitors: A review of 2002-2008 patents. Expert Opin. Ther. Patents 2009, 19, 1193-1228.
-
(2009)
Expert Opin. Ther. Patents
, vol.19
, pp. 1193-1228
-
-
Ramalho, T.C.1
Rocha, M.V.J.2
da Cunna, E.F.F.3
Freitas, M.P.4
-
46
-
-
41649085357
-
Design, synthesis, and biological evaluation of 1-(4-sulfamylphenyl)-3- trifluoromethyl-5-indolyl pyrazolines as cyclooxygenase-2 (COX-2) and lipoxygenase (LOX) inhibitors
-
Reddy, M. V. R.; Billa, V. K.; Pallela, V. R.; Mallireddigari, M. R.; Boominathan, R.; Gabriel, J. L.; Reddy, E. P. Design, synthesis, and biological evaluation of 1-(4-sulfamylphenyl)-3- trifluoromethyl-5-indolyl pyrazolines as cyclooxygenase-2 (COX-2) and lipoxygenase (LOX) inhibitors. Bioorg. Med. Chem. 2008, 16, 3907-3916.
-
(2008)
Bioorg. Med. Chem
, vol.16
, pp. 3907-3916
-
-
Reddy, M.V.R.1
Billa, V.K.2
Pallela, V.R.3
Mallireddigari, M.R.4
Boominathan, R.5
Gabriel, J.L.6
Reddy, E.P.7
-
47
-
-
41149169695
-
Computer-aided discovery of anti-inflammatory thiazolidinones with dual cyclooxygenase/lipoxygenase inhibition
-
Geronikaki, A. A.; Lagunin, A. A.; Hadjipavlou-Litina, D. I.; Eleftheriou, P. T.; Filimonov, D. A.; Poroikov, V. V.; Alam, I.; Saxena, A. K. Computer-aided discovery of anti-inflammatory thiazolidinones with dual cyclooxygenase/lipoxygenase inhibition. J. Med. Chem. 2008, 51, 1601-1609.
-
(2008)
J. Med. Chem
, vol.51
, pp. 1601-1609
-
-
Geronikaki, A.A.1
Lagunin, A.A.2
Hadjipavlou-Litina, D.I.3
Eleftheriou, P.T.4
Filimonov, D.A.5
Poroikov, V.V.6
Alam, I.7
Saxena, A.K.8
-
48
-
-
0032923356
-
12-Lipoxygenase: Classification, possible therapeutic benefits from inhibition and inhibitors
-
Dailey, L A.; Imming, P. 12-Lipoxygenase: Classification, possible therapeutic benefits from inhibition and inhibitors. Curr. Med. Chem. 1999, 6, 389-398.
-
(1999)
Curr. Med. Chem
, vol.6
, pp. 389-398
-
-
Dailey, L.A.1
Imming, P.2
-
49
-
-
71949100559
-
Synthesis and biological evaluation of salicylic acid and N-acetyl-2- carboxybenzenesulfonamide regioisomers possessing a N-difluoromethyl-1,2-dihydropyrid-2-one pharmacophore: Dual inhibitors of cyclooxygenases and 5-lipoxygenase with anti-inflammatory activity
-
Chowdhury, M. A.; Abdellatif, K. R.; Dong, Y.; Das, D.; Yu, G.; Velázquez, C. A.; Suresh, M. R.; Knaus, E. E. Synthesis and biological evaluation of salicylic acid and N-acetyl-2- carboxybenzenesulfonamide regioisomers possessing a N-difluoromethyl-1,2-dihydropyrid-2-one pharmacophore: dual inhibitors of cyclooxygenases and 5-lipoxygenase with anti-inflammatory activity. Bioorg. Med. Chem. 2009, 19, 6855-6861.
-
(2009)
Bioorg. Med. Chem
, vol.19
, pp. 6855-6861
-
-
Chowdhury, M.A.1
Abdellatif, K.R.2
Dong, Y.3
Das, D.4
Yu, G.5
Velázquez, C.A.6
Suresh, M.R.7
Knaus, E.E.8
-
50
-
-
64349120396
-
Synthesis of celecoxib analogues possessing a N-difluoromethyl-1,2-dihydropyrid-2-one 5-lipoxygenase pharmacophore: Biological evaluation as dual inhibitors of cyclooxygenases and 5-lipoxygenase with anti-inflammatory activity
-
Chowdhury, M. A.; Abdellatif, K. R.; Dong, Y.; Das, D.; Suresh, M. R.; Knaus, E. E. Synthesis of celecoxib analogues possessing a N-difluoromethyl-1,2-dihydropyrid-2-one 5-lipoxygenase pharmacophore: Biological evaluation as dual inhibitors of cyclooxygenases and 5-lipoxygenase with anti-inflammatory activity. J. Med. Chem. 2009, 52, 1525-1529.
-
(2009)
J. Med. Chem
, vol.52
, pp. 1525-1529
-
-
Chowdhury, M.A.1
Abdellatif, K.R.2
Dong, Y.3
Das, D.4
Suresh, M.R.5
Knaus, E.E.6
-
51
-
-
74549122427
-
Phenylacetic acid regioisomers possessing a N-difluoromethyl-1,2- dihydropyrid-2-one pharmacophore: Evaluation as dual inhibitors of cyclooxygenases and 5- lipoxygenase with anti-inflammatory activity
-
Yu, G.; Chowdhury, M. A.; Abdellatif, K. R.; Dong, Y.; Rao, P. N. P.; Das, D.; Velázquez, C. A.; Suresh, M. R.; Knaus, E. E. Phenylacetic acid regioisomers possessing a N-difluoromethyl-1,2- dihydropyrid-2-one pharmacophore: Evaluation as dual inhibitors of cyclooxygenases and 5- lipoxygenase with anti-inflammatory activity. Bioorg. Med. Chem. 2010, 20, 896-902.
-
(2010)
Bioorg. Med. Chem
, vol.20
, pp. 896-902
-
-
Yu, G.1
Chowdhury, M.A.2
Abdellatif, K.R.3
Dong, Y.4
Rao, P.N.P.5
Das, D.6
Velázquez, C.A.7
Suresh, M.R.8
Knaus, E.E.9
-
52
-
-
76449120588
-
Discovery of 3-(4-bromophenyl)-6-nitrobenzo[1.3.2]dithiazolium ylide 1,1-dioxide as a novel dual cyclooxygenase/5-lipoxygenase inhibitor that also inhibits tumor necrosis factor-alpha production
-
Chen, C. S.; Tan, C. M.; Huang, C. H.; Chang, L. C.; Wang, J. P.; Cheng, F. C.; Chern, J. W. Discovery of 3-(4-bromophenyl)-6-nitrobenzo[1.3.2]dithiazolium ylide 1,1-dioxide as a novel dual cyclooxygenase/5-lipoxygenase inhibitor that also inhibits tumor necrosis factor-alpha production. Bioorg. Med. Chem. 2010, 18, 597-604.
-
(2010)
Bioorg. Med. Chem
, vol.18
, pp. 597-604
-
-
Chen, C.S.1
Tan, C.M.2
Huang, C.H.3
Chang, L.C.4
Wang, J.P.5
Cheng, F.C.6
Chern, J.W.7
-
53
-
-
0032948111
-
Regulation and inhibition of phospholipase A2
-
Balsinde, J.; Balboa, M. A.; Insel, P. A.; Dennis, E. A. Regulation and inhibition of phospholipase A2. Annu. Rev. Pharmacol. Toxicol. 1999, 39, 175-189.
-
(1999)
Annu. Rev. Pharmacol. Toxicol
, vol.39
, pp. 175-189
-
-
Balsinde, J.1
Balboa, M.A.2
Insel, P.A.3
Dennis, E.A.4
-
54
-
-
0019789918
-
A specific acetylhydrolase for 1-alkyl-2-acetylsn- glycero-3-phosphocholine (a hypotensive and platelet-activating lipid)
-
Blank, M. L.; Lee, T.; Fitzgerald, V.; Snyder, F. A specific acetylhydrolase for 1-alkyl-2-acetylsn- glycero-3-phosphocholine (a hypotensive and platelet-activating lipid). J. Biol. Chem. 1981, 256, 175-178.
-
(1981)
J. Biol. Chem
, vol.256
, pp. 175-178
-
-
Blank, M.L.1
Lee, T.2
Fitzgerald, V.3
Snyder, F.4
-
55
-
-
0035190081
-
Evidence for a role of phospholipid oxidation products in atherogenesis
-
Berliner, J. A.; Subbanagounder, G.; Leitinger, N.; Watson, A.D.; Vora, D. Evidence for a role of phospholipid oxidation products in atherogenesis. Trends Cardiovasc. Med. 2001, 11, 142-147.
-
(2001)
Trends Cardiovasc. Med
, vol.11
, pp. 142-147
-
-
Berliner, J.A.1
Subbanagounder, G.2
Leitinger, N.3
Watson, A.D.4
Vora, D.5
-
56
-
-
0028785408
-
Plasma platelet-activating factor acetylhydrolase is a secreted phospholipase A2 with a catalytic triad
-
Tjoelker, L. W.; Eberhardt, C.; Unger, J.; Trong, H. L.; Zimmerman, G. A.; McIntyre, T. M.; Stafforini, D. M.; Prescott, S. M.; Gray, P. W. Plasma platelet-activating factor acetylhydrolase is a secreted phospholipase A2 with a catalytic triad. J. Biol. Chem. 1995, 270, 25481-25487.
-
(1995)
J. Biol. Chem
, vol.270
, pp. 25481-25487
-
-
Tjoelker, L.W.1
Eberhardt, C.2
Unger, J.3
Trong, H.L.4
Zimmerman, G.A.5
McIntyre, T.M.6
Stafforini, D.M.7
Prescott, S.M.8
Gray, P.W.9
-
57
-
-
33644837920
-
Role of lipoprotein-associated phospholipase A2 in atherosclerosis and its potential as a therapeutic target
-
Macphee, C. H.; Nelson, J.; Zalewski, A. Role of lipoprotein-associated phospholipase A2 in atherosclerosis and its potential as a therapeutic target. Curr. Opin. Pharmacol. 2006, 6, 154-161.
-
(2006)
Curr. Opin. Pharmacol
, vol.6
, pp. 154-161
-
-
Macphee, C.H.1
Nelson, J.2
Zalewski, A.3
-
58
-
-
0028968049
-
Anti-inflammatory properties of a platelet-activating factor acetylhydrolase
-
Tjoelker, L. W.; Wilder, C.; Eberhardt, C.; Stafforini, D. M.; Dietsch, G.; Schimpf, B.; Hooper, S.; Le Trong, H.; Cousens, L. S.; Zimmerman, G. A.; Yamadat, Y.; McIntyre, T. M.; Prescot, S. M.; Gray, P. W. Anti-inflammatory properties of a platelet-activating factor acetylhydrolase. Nature 1995, 374, 549-553.
-
(1995)
Nature
, vol.374
, pp. 549-553
-
-
Tjoelker, L.W.1
Wilder, C.2
Eberhardt, C.3
Stafforini, D.M.4
Dietsch, G.5
Schimpf, B.6
Hooper, S.7
le Trong, H.8
Cousens, L.S.9
Zimmerman, G.A.10
Yamadat, Y.11
McIntyre, T.M.12
Prescot, S.M.13
Gray, P.W.14
-
59
-
-
64749100269
-
The role of lipoprotein-associated phospholipase A2 in atherosclerosis may depend on its lipoprotein carrier in plasma
-
Tellis, C. C.; Tselepsis, A. D. The role of lipoprotein-associated phospholipase A2 in atherosclerosis may depend on its lipoprotein carrier in plasma. Biochim. Biophys. Acta 2009, 1791, 327-338.
-
(2009)
Biochim. Biophys. Acta
, vol.1791
, pp. 327-338
-
-
Tellis, C.C.1
Tselepsis, A.D.2
-
60
-
-
27944503521
-
Lipoprotein-associated phospholipase A2 as a biomarker for coronary disease and stroke
-
Caslake, M. J.; Packard, C. J. Lipoprotein-associated phospholipase A2 as a biomarker for coronary disease and stroke. Nat. Rev. Cardiol. 2005, 2, 529-535.
-
(2005)
Nat. Rev. Cardiol
, vol.2
, pp. 529-535
-
-
Caslake, M.J.1
Packard, C.J.2
-
61
-
-
53549093853
-
Inhibition of lipoprotein-associated phospholipase A2 reduces complex coronary atherosclerotic plaque development
-
Wilensky, R. L.; Shi, Y.; Mohler, E. R.; Hamamdzic, D.; Burgert, M. E.; Li, J.; Postle, A.; Fenning, R. S.; Bollinger, J. G.; Hoffman, B. E.; Pelchovitz, D. J.; Yang, J.; Mirabile, R. C.; Webb, C. L.; Zhang, L.; Zhang, P.; Gelb, M. H.; Walker, M. C.; Zalewski, A.; Macphee, C. H. Inhibition of lipoprotein-associated phospholipase A2 reduces complex coronary atherosclerotic plaque development. Nat. Med. 2008, 14, 1059-1066.
-
(2008)
Nat. Med
, vol.14
, pp. 1059-1066
-
-
Wilensky, R.L.1
Shi, Y.2
Mohler, E.R.3
Hamamdzic, D.4
Burgert, M.E.5
Li, J.6
Postle, A.7
Fenning, R.S.8
Bollinger, J.G.9
Hoffman, B.E.10
Pelchovitz, D.J.11
Yang, J.12
Mirabile, R.C.13
Webb, C.L.14
Zhang, L.15
Zhang, P.16
Gelb, M.H.17
Walker, M.C.18
Zalewski, A.19
Macphee, C.H.20
more..
-
62
-
-
18244373708
-
Role of lipoprotein-associated phospholipase A2 in atherosclerosis: Biology, epidemiology, and possible therapeutic target
-
Zalewski, A.; Nelson, J. J.; Hegg, L.; Macphee, C. Role of lipoprotein-associated phospholipase A2 in atherosclerosis: Biology, epidemiology, and possible therapeutic target. Arterioscler. Thromb. Vasc. Biol. 2005, 25, 923-931.
-
(2005)
Arterioscler. Thromb. Vasc. Biol
, vol.25
, pp. 923-931
-
-
Zalewski, A.1
Nelson, J.J.2
Hegg, L.3
Macphee, C.4
-
63
-
-
33846858869
-
Role of lipoprotein-associated phospholipase A2 in leukocyte activation and inflammatory responses
-
Shi, Y.; Zhang, P.; Zhang, L.; Osman, H.; Mohler, E. R.; Macpheec, C.; Zalewski, A.; Postle, A.; Wilensky, R. L. Role of lipoprotein-associated phospholipase A2 in leukocyte activation and inflammatory responses. Atherosclerosis 2007, 191, 54-62.
-
(2007)
Atherosclerosis
, vol.191
, pp. 54-62
-
-
Shi, Y.1
Zhang, P.2
Zhang, L.3
Osman, H.4
Mohler, E.R.5
Macpheec, C.6
Zalewski, A.7
Postle, A.8
Wilensky, R.L.9
-
64
-
-
33748288122
-
Lp-PLA2: A new kid on the block
-
Zalewski, A.; Nelson, J. J.; Heg, J. J. Macphee, C. Lp-PLA2: A new kid on the block. Clin. Chem. 2006, 52, 1645-1649.
-
(2006)
Clin. Chem
, vol.52
, pp. 1645-1649
-
-
Zalewski, A.1
Nelson, J.J.2
Heg, J.J.3
Macphee, C.4
-
65
-
-
33947732957
-
Discovery of ecopladib, an indole inhibitor of cytosolic phospholipase A2α
-
Lee, K. L.; Foley, M. A.; Chen, L.; Behnke, M. L.; Lovering, F. E.; Kirincich, S. J.; Wang, W.; Shim, J.; Tam, S.; Shen, M. W.; Khor, S.; Xu, X.; Goodwin, D. G.; Ramarao, M. K.; Nickerson- Nutter, C.; Donahue, F.; Ku, M. S.; Clark, J. D.; McKew, J. C. Discovery of ecopladib, an indole inhibitor of cytosolic phospholipase A2α. J. Med. Chem. 2007, 50, 1380-1400.
-
(2007)
J. Med. Chem
, vol.50
, pp. 1380-1400
-
-
Lee, K.L.1
Foley, M.A.2
Chen, L.3
Behnke, M.L.4
Lovering, F.E.5
Kirincich, S.J.6
Wang, W.7
Shim, J.8
Tam, S.9
Shen, M.W.10
Khor, S.11
Xu, X.12
Goodwin, D.G.13
Ramarao, M.K.14
Nickerson-Nutter, C.15
Donahue, F.16
Ku, M.S.17
Clark, J.D.18
McKew, J.C.19
-
66
-
-
70349319716
-
Phospholipase A2 inhibitors in the treatment of atherosclerosis: A new approach moves forward in the clinic
-
Suckling, K. E. Phospholipase A2 inhibitors in the treatment of atherosclerosis: A new approach moves forward in the clinic. Expert Opin. Investig. Drugs. 2009, 18, 1425-1430.
-
(2009)
Expert Opin. Investig. Drugs
, vol.18
, pp. 1425-1430
-
-
Suckling, K.E.1
-
67
-
-
60249101701
-
Effects of 1-H-indole-3-glyoxamide (A-002) on concentration of secretory phospholipase A2 (PLASMA study): A phase II double-blind, randomized, placebo-controlled trial
-
Rosenson, R. S.; Hislop, C.; McConnell, D.; Elliott, M.; Stasiv, Y.; Wang, N., Waters, D. D. Effects of 1-H-indole-3-glyoxamide (A-002) on concentration of secretory phospholipase A2 (PLASMA study): A phase II double-blind, randomized, placebo-controlled trial. Lancet 2009, 373, 649-658.
-
(2009)
Lancet
, vol.373
, pp. 649-658
-
-
Rosenson, R.S.1
Hislop, C.2
McConnell, D.3
Elliott, M.4
Stasiv, Y.5
Wang, N.6
Waters, D.D.7
-
68
-
-
60249083241
-
Phospholipase A2 inhibitors in atherosclerosis: The race is on
-
Corson, M. A.; Phospholipase A2 inhibitors in atherosclerosis: The race is on. Lancet 2009, 373, 608-610.
-
(2009)
Lancet
, vol.373
, pp. 608-610
-
-
Corson, M.A.1
-
69
-
-
0032516463
-
Mechanism of inhibition of LDL phospholipase A2 by monocyclic beta-lactams: Burst kinetics and the effect of stereochemistry
-
Tew, D. G.; Boyd, H. F.; Ashman, S.; Theobald, C.; Leach, C. A. Mechanism of inhibition of LDL phospholipase A2 by monocyclic beta-lactams: Burst kinetics and the effect of stereochemistry. Biochemistry 1998, 37, 10087-10093.
-
(1998)
Biochemistry
, vol.37
, pp. 10087-10093
-
-
Tew, D.G.1
Boyd, H.F.2
Ashman, S.3
Theobald, C.4
Leach, C.A.5
-
70
-
-
0037463766
-
The identification of clinical candidate SB-480848: A potent inhibitor of lipoprotein-associated phospholipase A2
-
Blackie, J. A.; Bloomer, J. C.; Brown, M. J.; Cheng, H. Y.; Hammond, B.; Hickey, D. M.; Ife, R. J.; Leach, C. A.; Lewis, V. A.; Macphee, C. H.; Milliner, K. J.; Moores, K. E.; Pinto, I. L.; Smith, S. A.; Stansfield, I. G.; Stanway, S. J.; Taylor, M. A.; Theobald, C. J. The identification of clinical candidate SB-480848: A potent inhibitor of lipoprotein-associated phospholipase A2. Bioorg. Med. Chem. Lett. 2003, 13, 1067-1070.
-
(2003)
Bioorg. Med. Chem. Lett
, vol.13
, pp. 1067-1070
-
-
Blackie, J.A.1
Bloomer, J.C.2
Brown, M.J.3
Cheng, H.Y.4
Hammond, B.5
Hickey, D.M.6
Ife, R.J.7
Leach, C.A.8
Lewis, V.A.9
Macphee, C.H.10
Milliner, K.J.11
Moores, K.E.12
Pinto, I.L.13
Smith, S.A.14
Stansfield, I.G.15
Stanway, S.J.16
Taylor, M.A.17
Theobald, C.J.18
-
71
-
-
77954934110
-
N-Substituted pyridinone and pyrimidinone derivatives for use as Lp- PLA2 inhibitors in the treatment atherosclerosis
-
WO 03/086400
-
Leach, C. A.; Smith, S. A. N-Substituted pyridinone and pyrimidinone derivatives for use as Lp- PLA2 inhibitors in the treatment atherosclerosis. World Patent 2003, WO 03/086400, 1-33.
-
(2003)
World Patent
, pp. 1-33
-
-
Leach, C.A.1
Smith, S.A.2
-
72
-
-
43049122963
-
The effect of darapladib on plasma lipoprotein-associated phospholipase A2 activity and cardiovascular biomarkers in patients with stable coronary heart disease or coronary heart disease risk equivalent: The results of a multicenter, randomized, double-blind, placebo-controlled study
-
Mohler, E. R.; Ballantyne, C. M.; Davidson, M. H.; Hanefeld, M.; Ruilope, L. M.; Johnson, J. L.; Zalewski, A. The effect of darapladib on plasma lipoprotein-associated phospholipase A2 activity and cardiovascular biomarkers in patients with stable coronary heart disease or coronary heart disease risk equivalent: The results of a multicenter, randomized, double-blind, placebo-controlled study. J. Am. Coll. Cardiol. 2008, 51, 1632-1641.
-
(2008)
J. Am. Coll. Cardiol
, vol.51
, pp. 1632-1641
-
-
Mohler, E.R.1
Ballantyne, C.M.2
Davidson, M.H.3
Hanefeld, M.4
Ruilope, L.M.5
Johnson, J.L.6
Zalewski, A.7
-
73
-
-
58549103715
-
Future role for selective phospholipase A2 inhibitors in the prevention of atherosclerotic cardiovascular disease
-
Rosenson, R. S. Future role for selective phospholipase A2 inhibitors in the prevention of atherosclerotic cardiovascular disease. Cardiovasc. Drugs Ther. 2009, 23, 93-101.
-
(2009)
Cardiovasc. Drugs Ther
, vol.23
, pp. 93-101
-
-
Rosenson, R.S.1
-
74
-
-
68449083214
-
Darapladib and atherosclerotic plaque: Should lipoprotein-associated phospholipase A2 be a therapeutic target
-
McCullough, P. A. Darapladib and atherosclerotic plaque: Should lipoprotein-associated phospholipase A2 be a therapeutic target? Curr. Atherosclerosis Rep. 2009, 11, 334-337.
-
(2009)
Curr. Atherosclerosis Rep
, vol.11
, pp. 334-337
-
-
McCullough, P.A.1
-
75
-
-
0033011878
-
Common structural features of MAPEG-A widespread superfamily of membrane associated proteins with highly divergent functions in eicosanoid and glutathione metabolism
-
Jakobsson, P. J.; Morgenstern, R.; Mancini, J.; Ford-Hutchinson, A.; Persson, B. Common structural features of MAPEG-A widespread superfamily of membrane associated proteins with highly divergent functions in eicosanoid and glutathione metabolism. Protein Sci. 1999, 8, 689-692.
-
(1999)
Protein Sci
, vol.8
, pp. 689-692
-
-
Jakobsson, P.J.1
Morgenstern, R.2
Mancini, J.3
Ford-Hutchinson, A.4
Persson, B.5
-
76
-
-
0033594963
-
Identification of human prostaglandin E synthase: A microsomal, glutathione-dependent, inducible enzyme, constituting a potential novel drug target
-
Jakobsson, P. J.; Thorén, S.; Morgenstern, R.; Samuelsson B. Identification of human prostaglandin E synthase: A microsomal, glutathione-dependent, inducible enzyme, constituting a potential novel drug target. Proc. Natl. Acad. Sci. USA 1999, 96, 7220-7225.
-
(1999)
Proc. Natl. Acad. Sci. USA
, vol.96
, pp. 7220-7225
-
-
Jakobsson, P.J.1
Thorén, S.2
Morgenstern, R.3
Samuelsson, B.4
-
77
-
-
34748817976
-
Membrane prostaglandin E synthase-1: A novel therapeutic target
-
Samuelsson, B.; Morgenstern, R.; Jakobsson, P. J. Membrane prostaglandin E synthase-1: A novel therapeutic target. Pharmacol. Rev. 2007, 59, 207-224.
-
(2007)
Pharmacol. Rev
, vol.59
, pp. 207-224
-
-
Samuelsson, B.1
Morgenstern, R.2
Jakobsson, P.J.3
-
78
-
-
47749092391
-
Microsomal prostaglandin E2 synthase-1 (mPGES-1): A novel antiinflammatory therapeutic target
-
Friesen, R. W.; Mancini, J. A. Microsomal prostaglandin E2 synthase-1 (mPGES-1): A novel antiinflammatory therapeutic target. J. Med. Chem. 2008, 51, 4059-4067.
-
(2008)
J. Med. Chem
, vol.51
, pp. 4059-4067
-
-
Friesen, R.W.1
Mancini, J.A.2
-
79
-
-
49649104307
-
Structural basis for induced formation of the inflammatory mediator prostaglandin E2
-
Jegerschoeld, C.; Pawelzik, S.-C.; Purhonen, P.; Bhakat, P.; Gheorghe, K. R.; Gyobu, N.; Mitsuoka, K.; Morgenstern, R.; Jakobsson, P. J.; Hebert, H. Structural basis for induced formation of the inflammatory mediator prostaglandin E2. Proc. Natl. Acad. Sci. USA 2009, 105, 11110-11115.
-
(2009)
Proc. Natl. Acad. Sci. USA
, vol.105
, pp. 11110-11115
-
-
Jegerschoeld, C.1
Pawelzik, S.-C.2
Purhonen, P.3
Bhakat, P.4
Gheorghe, K.R.5
Gyobu, N.6
Mitsuoka, K.7
Morgenstern, R.8
Jakobsson, P.J.9
Hebert, H.10
-
80
-
-
20644467057
-
Inhibitors of the inducible microsomal prostaglandin E2 synthase (mPGES-1) derived from MK-886
-
Riendeau, D.; Aspiotis, R.; Ethier, D.; Gareau, Y.; Grimm, E. L.; Guay, J.; Guiral, S.; Juteau, H.; Mancini, J. A.; Méthot, N.; Rubin, J.; Friesen, R. W. Inhibitors of the inducible microsomal prostaglandin E2 synthase (mPGES-1) derived from MK-886. Bioorg. Med. Chem. Lett. 2005, 15, 3352-3355.
-
(2005)
Bioorg. Med. Chem. Lett
, vol.15
, pp. 3352-3355
-
-
Riendeau, D.1
Aspiotis, R.2
Ethier, D.3
Gareau, Y.4
Grimm, E.L.5
Guay, J.6
Guiral, S.7
Juteau, H.8
Mancini, J.A.9
Méthot, N.10
Rubin, J.11
Friesen, R.W.12
-
81
-
-
35848954713
-
Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors
-
Côté, B.; Boulet, L.; Brideau, C.; Claveau, D.; Ethier, D.; Frenette, R.; Gagnon, M.; Giroux, A.; Guay, J.; Guiral, S.; Mancini, J.; Martins, E.; Massé, F.; Méthot, N.; Riendeau, D.; Rubin, J.; Xu, D.; Yu, H.; Ducharme, Y.; Friesen, R. W. Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors. Bioorg. Med. Chem. Lett. 2007, 17, 6816-6820.
-
(2007)
Bioorg. Med. Chem. Lett
, vol.17
, pp. 6816-6820
-
-
Côté, B.1
Boulet, L.2
Brideau, C.3
Claveau, D.4
Ethier, D.5
Frenette, R.6
Gagnon, M.7
Giroux, A.8
Guay, J.9
Guiral, S.10
Mancini, J.11
Martins, E.12
Massé, F.13
Méthot, N.14
Riendeau, D.15
Rubin, J.16
Xu, D.17
Yu, H.18
Ducharme, Y.19
Friesen, R.W.20
more..
-
82
-
-
70349226756
-
Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors
-
Giroux, A.; Boulet, L.; Brideau, C.; Chau, A.; Claveau, D.; Côté, B.; Ethier, D.; Frenette, R.; Gagnon, M.; Guay, J.; Guiral, S.; Mancini, J.; Martins, E.; Massé, F.; Méthot, N.; Riendeau, D.; Rubin, J.; Xu, D.; Yu, H.; Ducharme, Y.; Friesen, R. W. Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors. Bioorg. Med. Chem. Lett. 2009, 19, 5837-5841.
-
(2009)
Bioorg. Med. Chem. Lett
, vol.19
, pp. 5837-5841
-
-
Giroux, A.1
Boulet, L.2
Brideau, C.3
Chau, A.4
Claveau, D.5
Côté, B.6
Ethier, D.7
Frenette, R.8
Gagnon, M.9
Guay, J.10
Guiral, S.11
Mancini, J.12
Martins, E.13
Massé, F.14
Méthot, N.15
Riendeau, D.16
Rubin, J.17
Xu, D.18
Yu, H.19
Ducharme, Y.20
Friesen, R.W.21
more..
-
83
-
-
58149097590
-
Pirinixic acid derivatives as novel dual inhibitors of microsomal prostaglandin E2 synthase-1 and 5- lipoxygenase
-
Koeberle, A.; Zettl, H.; Greiner, C.; Wurglics, M.; Schubert-Zsilavecz, M.; Werz, O. Pirinixic acid derivatives as novel dual inhibitors of microsomal prostaglandin E2 synthase-1 and 5- lipoxygenase. J. Med. Chem. 2008, 51, 8068-8076.
-
(2008)
J. Med. Chem
, vol.51
, pp. 8068-8076
-
-
Koeberle, A.1
Zettl, H.2
Greiner, C.3
Wurglics, M.4
Schubert-Zsilavecz, M.5
Werz, O.6
-
84
-
-
0025132245
-
Activation of a member of the steroid hormone receptor superfamily by peroxisome proliferators
-
Issemann, I.; Green, S. Activation of a member of the steroid hormone receptor superfamily by peroxisome proliferators. Nature 1990, 347, 645-650.
-
(1990)
Nature
, vol.347
, pp. 645-650
-
-
Issemann, I.1
Green, S.2
-
85
-
-
0030854677
-
PPAR alpha structure-function relationships derived from species-specific differences in responsiveness to hypolipidemic agents
-
Keller, H.; Devchand, P. R.; Perroud, M.; Wahli, W. PPAR alpha structure-function relationships derived from species-specific differences in responsiveness to hypolipidemic agents. Biol. Chem. 1997, 378, 651-655.
-
(1997)
Biol. Chem
, vol.378
, pp. 651-655
-
-
Keller, H.1
Devchand, P.R.2
Perroud, M.3
Wahli, W.4
-
86
-
-
68549088901
-
Arylpyrrolizines as inhibitors of microsomal prostaglandin E2 synthase-1 (mPGES-1) or as dual inhibitors of mPGES-1 and 5-lipoxygenase (5-LOX)
-
Liedtke, A. J.; Keck, P. R.; Lehmann, F.; Koeberle, A.; Werz, O.; Laufer, S. A. Arylpyrrolizines as inhibitors of microsomal prostaglandin E2 synthase-1 (mPGES-1) or as dual inhibitors of mPGES-1 and 5-lipoxygenase (5-LOX). J. Med. Chem. 2009, 52, 4968-4972.
-
(2009)
J. Med. Chem
, vol.52
, pp. 4968-4972
-
-
Liedtke, A.J.1
Keck, P.R.2
Lehmann, F.3
Koeberle, A.4
Werz, O.5
Laufer, S.A.6
-
87
-
-
77249100287
-
Nonacidic inhibitors of human microsomal prostaglandin synthase 1 (mPGES 1) identified by a multistep virtual screening protocol
-
Rörsch, F.; Wobst, I.; Zettl, H.; Schubert-Zsilavecz, M.; Grösch, S.; Geisslinger, G.; Schneider, G.; Proschak, E. Nonacidic inhibitors of human microsomal prostaglandin synthase 1 (mPGES 1) identified by a multistep virtual screening protocol. J. Med. Chem. 2010, 53, 911-915.
-
(2010)
J. Med. Chem
, vol.53
, pp. 911-915
-
-
Rörsch, F.1
Wobst, I.2
Zettl, H.3
Schubert-Zsilavecz, M.4
Grösch, S.5
Geisslinger, G.6
Schneider, G.7
Proschak, E.8
-
88
-
-
76649142022
-
Selective inducible microsomal prostaglandin E(2) synthase-1 (mPGES-1) inhibitors derived from an oxicam template
-
Wang, J.; Limburg, D.; Carter, J.; Mbalaviele, G.; Gierse, J.; Vazquez, M. Selective inducible microsomal prostaglandin E(2) synthase-1 (mPGES-1) inhibitors derived from an oxicam template. Bioorg. Med. Chem. Lett. 2010, 20, 1604-1609.
-
(2010)
Bioorg. Med. Chem. Lett
, vol.20
, pp. 1604-1609
-
-
Wang, J.1
Limburg, D.2
Carter, J.3
Mbalaviele, G.4
Gierse, J.5
Vazquez, M.6
-
89
-
-
0142218524
-
Prospects for the development of small molecular weight compounds to replace anti-tumour necrosis factor biological agents
-
Foxwell, B.; Andreakos, E.; Brennan, F.; Feldmann, M.; Smith, C.; Conron, M. Prospects for the development of small molecular weight compounds to replace anti-tumour necrosis factor biological agents. Ann. Rheum. Dis. 2003, 62, ii90-ii93.
-
(2003)
Ann. Rheum. Dis
, vol.62
-
-
Foxwell, B.1
Andreakos, E.2
Brennan, F.3
Feldmann, M.4
Smith, C.5
Conron, M.6
-
90
-
-
37249004920
-
Reaching for high-hanging fruit in drug discovery at proteinprotein interfaces
-
Wells, J. A.; McClendon, C. L. Reaching for high-hanging fruit in drug discovery at proteinprotein interfaces. Nature 2007, 450, 1001-1009.
-
(2007)
Nature
, vol.450
, pp. 1001-1009
-
-
Wells, J.A.1
McClendon, C.L.2
-
91
-
-
34347376515
-
The future of TNF-α antagonism
-
Taylor, P. C. The future of TNF-α antagonism. Future Rheumatol. 2007, 2, 233-236.
-
(2007)
Future Rheumatol
, vol.2
, pp. 233-236
-
-
Taylor, P.C.1
-
92
-
-
27744586067
-
Small-molecule inhibition of TNF-alpha
-
He, M. M.; Smith, A. S.; Oslob, J. D.; Flanagan, W. M.; Braisted, A. C.; Whitty, A.; Cancilla, M. T.; Wang, J.; Lugovskoy, A. A.; Yoburn, J. C.; Fung, A. D.; Farrington, G.; Eldredge, J. K.; Day, E. S.; Cruz, L. A.; Cachero, T. G.; Miller, S. K.; Friedman, J. E.; Choong, I. C.; Cunningham, B. C. Small-molecule inhibition of TNF-alpha. Science 2005, 310, 1022-1025.
-
(2005)
Science
, vol.310
, pp. 1022-1025
-
-
He, M.M.1
Smith, A.S.2
Oslob, J.D.3
Flanagan, W.M.4
Braisted, A.C.5
Whitty, A.6
Cancilla, M.T.7
Wang, J.8
Lugovskoy, A.A.9
Yoburn, J.C.10
Fung, A.D.11
Farrington, G.12
Eldredge, J.K.13
Day, E.S.14
Cruz, L.A.15
Cachero, T.G.16
Miller, S.K.17
Friedman, J.E.18
Choong, I.C.19
Cunningham, B.C.20
more..
-
93
-
-
64349119966
-
Discovery of (S)-N-[2-[1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethyl]-1,3-dioxo-2,3- dihydro-1H-isoindol-4-yl] acetamide (apremilast), a potent and orally active phosphodiesterase 4 and tumor necrosis factor-alpha inhibitor
-
Man, H. W.; Schafer, P.; Wong, L. M.; Patterson, R. T.; Corral, L. G.; Raymon, H.; Blease, K.; Leisten, J.; Shirley, M. A.; Tang, Y.; Babusis, D. M.; Chen, R.; Stirling, D.; Muller, G. W. Discovery of (S)-N-[2-[1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethyl]-1,3-dioxo-2,3- dihydro-1H-isoindol-4-yl] acetamide (apremilast), a potent and orally active phosphodiesterase 4 and tumor necrosis factor-alpha inhibitor. J. Med. Chem. 2009, 52, 1522-1524.
-
(2009)
J. Med. Chem
, vol.52
, pp. 1522-1524
-
-
Man, H.W.1
Schafer, P.2
Wong, L.M.3
Patterson, R.T.4
Corral, L.G.5
Raymon, H.6
Blease, K.7
Leisten, J.8
Shirley, M.A.9
Tang, Y.10
Babusis, D.M.11
Chen, R.12
Stirling, D.13
Muller, G.W.14
-
94
-
-
77950498477
-
Structure-based discovery of natural-product-like TNF-α inhibitors
-
Chan, D. S.; Lee, H. M.; Yang, F.; Che, C. M.; Wong, C. C. L.; Abagyan, R.; Leung, C. H.; Ma, D. L. Structure-based discovery of natural-product-like TNF-α inhibitors. Angew. Chem. Int. Ed. 2010, 49, 2860-2864.
-
(2010)
Angew. Chem. Int. Ed
, vol.49
, pp. 2860-2864
-
-
Chan, D.S.1
Lee, H.M.2
Yang, F.3
Che, C.M.4
Wong, C.C.L.5
Abagyan, R.6
Leung, C.H.7
Ma, D.L.8
|