1 |
Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
|
2 |
Scaffold of the cyclooxygenase-2 (COX-2) inhibitor carprofen provides Alzheimer gamma-secretase modulators. J Med Chem. 2006 Dec 28;49(26):7588-91.
|
3 |
Pfizer. Product Development Pipeline. March 31 2009.
|
4 |
Celecoxib and rofecoxib. The role of COX-2 inhibitors in dental practice. J Am Dent Assoc. 2001 Apr;132(4):451-6.
|
5 |
Cox-2 inhibitory effects of naturally occurring and modified fatty acids. J Nat Prod. 2001 Jun;64(6):745-9.
|
6 |
Membranous nephropathy associated with the relatively selective cyclooxygenase-2 inhibitor, etodolac, in a patient with early rheumatoid arthritis. Intern Med. 2007;46(13):1055-8.
|
7 |
The effect of newer anti-rheumatic drugs on osteogenic cell proliferation: an in-vitro study. J Orthop Surg Res. 2009 May 26;4:17.
|
8 |
Fenbufen based 3-[5-(substituted aryl)-1,3,4-oxadiazol-2-yl]-1-(biphenyl-4-yl)propan-1-ones as safer antiinflammatory and analgesic agents. Eur J Med Chem. 2009 Sep;44(9):3798-804.
|
9 |
Ouellet M, Percival MD: Effect of inhibitor time-dependency on selectivity towards cyclooxygenase isoforms. Biochem J. 1995 Feb 15;306 ( Pt 1):247-51.
|
10 |
Flurbiprofen, a cyclooxygenase inhibitor, protects mice from hepatic ischemia/reperfusion injury by inhibiting GSK-3 signaling and mitochondrial permeability transition.Mol Med.2012 Sep 25;18:1128-35.
|
11 |
Maternal toxicity of nonsteroidal anti-inflammatory drugs as an important factor affecting prenatal development. Reprod Toxicol. 2009 Sep;28(2):239-44.
|
12 |
Probing the skin permeation of fish oil/EPA and ketoprofen-3. Effects on epidermal COX-2 and LOX. Prostaglandins Leukot Essent Fatty Acids. 2007 Jun;76(6):357-62.
|
13 |
Dissociation of airway inflammation and hyperresponsiveness by cyclooxygenase inhibition in allergen challenged mice. Eur Respir J. 2009 Jul;34(1):200-8.
|
14 |
Role of COX-2-derived metabolites in regulation of the renal hemodynamic response to norepinephrine. Am J Physiol Renal Physiol. 2001 Nov;281(5):F975-82.
|
15 |
Systematic pharmacological approach to the characterization of NSAIDs. Prostaglandins Leukot Essent Fatty Acids. 1998 Jul;59(1):55-62.
|
16 |
Meloxicam: selective COX-2 inhibition in clinical practice. Semin Arthritis Rheum. 1997 Jun;26(6 Suppl 1):21-7.
|
17 |
Renal effects of nabumetone, a COX-2 antagonist: impairment of function in isolated perfused rat kidneys contrasts with preserved renal function in vivo. Exp Nephrol. 2001;9(6):387-96.
|
18 |
Comparative inhibitory activity of rofecoxib, meloxicam, diclofenac, ibuprofen, and naproxen on COX-2 versus COX-1 in healthy volunteers. J Clin Pharmacol. 2000 Oct;40(10):1109-20.
|
19 |
Rat ovulation, implantation and decidualization are severely compromised by COX-2 inhibitors. Front Biosci. 2007 May 1;12:3333-42.
|
20 |
COX-1 and COX-2 inhibition in horse blood by phenylbutazone, flunixin, carprofen and meloxicam: an in vitro analysis. Pharmacol Res. 2005 Oct;52(4):302-6.
|
21 |
Privileged structures: a useful concept for the rational design of new lead drug candidates. Mini Rev Med Chem. 2007 Nov;7(11):1108-19.
|
22 |
The use and safety profile of non-steroidal antiinflammatory drugs among Turkish patients with osteoarthritis. Turk J Gastroenterol. 2005 Sep;16(3):138-42.
|
23 |
Effects of tiaprofenic acid on the concentration and metabolism of proteoglycans in normal and degenerating canine articular cartilage. J Clin Pharmacol. 1990 Sep;30(9):808-14.
|
24 |
Biochemical mechanisms of New Molecular Entities (NMEs) approved by United States FDA during 2001-2004: mechanisms leading to optimal efficacy and ... Curr Top Med Chem. 2006;6(5):461-78.
|
25 |
Synthesis and anti-inflammatory activity of the major metabolites of imrecoxib. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2270-2.
|
26 |
2-Arylpropionic CXC chemokine receptor 1 (CXCR1) ligands as novel noncompetitive CXCL8 inhibitors. J Med Chem. 2005 Jun 30;48(13):4312-31.
|
27 |
Pharmacokinetic, pharmacodynamic, and safety/tolerability profiles of CG100649, a novel COX-2 inhibitor: results of a phase i, randomized, multiple-dose study in healthy Korean men and women. Clin Ther. 2015 Jan 1;37(1):197-210.
|
28 |
Design, synthesis, biological evaluation and molecular docking of curcumin analogues as antioxidant, cyclooxygenase inhibitory and anti-inflammator... Bioorg Med Chem Lett. 2005 Apr 1;15(7):1793-7.
|
29 |
Topical NSAID therapy for musculoskeletal pain. Pain Med. 2010 Apr;11(4):535-49.
|
30 |
Novel dual cyclooxygenase and lipoxygenase inhibitors targeting hyaluronan-CD44v6 pathway and inducing cytotoxicity in colon cancer cells. Bioorg Med Chem. 2013 May 1;21(9):2551-9.
|
31 |
Pharmacokinetic profiles of the novel COX-2 selective inhibitor cimicoxib in dogs.Vet J.2014 Apr;200(1):77-81.
|
32 |
Effects of the COX-2 inhibitor FK3311 on ischemia - reperfusion injury in the rat lung. J Invest Surg. 2007 May-Jun;20(3):175-80.
|
33 |
Modeling and simulation to support dose selection and clinical development of SC-75416, a selective COX-2 inhibitor for the treatment of acute and ... Clin Pharmacol Ther. 2008 Jun;83(6):857-66.
|
34 |
National Cancer Institute Drug Dictionary (drug name CA102N).
|
35 |
Monocyte intracellular cytokine production during human endotoxaemia with or without a second in vitro LPS challenge: effect of RWJ-67657, a p38 MAP-kinase inhibitor, on LPS-hyporesponsiveness. Clin Exp Immunol. 2002 Feb;127(2):337-43.
|
36 |
Fatty acid amide hydrolase inhibitors: a patent review (2009-2014).Expert Opin Ther Pat. 2015;25(11):1247-66.
|
37 |
Gelatinase inhibitors: a patent review (2011-2017).Expert Opin Ther Pat. 2018 Jan;28(1):31-46.
|
38 |
Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.
|
39 |
Development of a botanical anti-arthritis drug, PMI-001. SBIR.STTR America's Seed Fund.
|
40 |
Dexketoprofene, selective cox-1 inhibitor nsaids, without gastrointestinal injury in rats. Acta Gastroenterol Latinoam. 2002 May;32(1):17-20.
|
41 |
Apricoxib, a COX-2 inhibitor for the potential treatment of pain and cancer. IDrugs. 2009 Nov;12(11):711-22.
|
42 |
ClinicalTrials.gov (NCT00506298) Study of CRx-401 on Glucose Levels in Subjects With Type II Diabetes. U.S. National Institutes of Health.
|
43 |
Clinical pipeline report, company report or official report of raqualia.
|
44 |
Effects of S-2474, a novel nonsteroidal anti-inflammatory drug, on amyloid beta protein-induced neuronal cell death. Br J Pharmacol. 2001 Oct;134(3):673-81.
|
45 |
New cyclooxygenase-2/5-lipoxygenase inhibitors. 2. 7-tert-butyl-2,3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflamm... J Med Chem. 1998 Mar 26;41(7):1124-37.
|
46 |
4-(4-cycloalkyl/aryl-oxazol-5-yl)benzenesulfonamides as selective cyclooxygenase-2 inhibitors: enhancement of the selectivity by introduction of a ... J Med Chem. 2002 Mar 28;45(7):1511-7.
|
47 |
Current status of COX-2 inhibitors. Mini Rev Med Chem. 2008 Jan;8(1):73-90.
|
48 |
Enantioselective HPLC determination of E-6087, a new COX-2 inhibitor, in human plasma: Validation and pharmacokinetic application. Chirality. 2004 May 15;16(5):302-8.
|
49 |
Role of cyclooxygenases 1 and 2 in the modulation of neuromuscular functions in the distal colon of humans and mice. Gut. 2005 May; 54(5): 608-616.
|
50 |
Effect of flosulide, a selective cyclooxygenase 2 inhibitor, on passive heymann nephritis in the rat. Kidney Int. 1999 Nov;56(5):1770-8.
|
51 |
Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007983)
|
52 |
Pharmacology of a selective cyclooxygenase-2 inhibitor, L-745,337: a novel nonsteroidal anti-inflammatory agent with an ulcerogenic sparing effect ... J Pharmacol Exp Ther. 1995 Sep;274(3):1531-7.
|
53 |
Characterization of the in vitro oxidative metabolites of the COX-2 selective inhibitor L-766,112. Bioorganic & Medicinal Chemistry Letters Volume 7, Issue 1, 7 January 1997, Pages 53-56.
|
54 |
Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.
|
55 |
Selective COX-2 Inhibitors: A Review of Their Structure-Activity Relationships. Iran J Pharm Res. 2011 Autumn; 10(4): 655-683.
|
56 |
New drugs in development for the treatment of endometriosis. Expert Opin Investig Drugs. 2008 Aug;17(8):1187-202.
|
57 |
The discovery of RPR 200765A, a p38 MAP kinase inhibitor displaying a good oral anti-arthritic efficacy. Bioorg Med Chem. 2001 Feb;9(2):537-54.
|
58 |
Evaluation of the antiinflammatory activity of a dual cyclooxygenase-2 selective/5-lipoxygenase inhibitor, RWJ 63556, in a canine model of inflammation. J Pharmacol Exp Ther. 1997 Aug;282(2):1094-101.
|
59 |
S 33516 Servier preclinical data. R & D Focus Drug News. July 12, 1999.
|
60 |
Inhibition of p38 MAP kinase as a therapeutic strategy. Immunopharmacology. 2000 May;47(2-3):185-201.
|
61 |
Cyclooxygenase (COX)-2-dependent effects of the inhibitor SC236 when combined with ionizing radiation in mammary tumor cells derived from HER-2/neu mice. Mol Cancer Ther. 2004 Apr;3(4):417-24.
|
62 |
Identification and optimisation of a novel series of pyrimidine based cyclooxygenase-2 (COX-2) inhibitors. Utilisation of a biotransformation appro... Bioorg Med Chem Lett. 2009 Aug 1;19(15):4509-14.
|
63 |
Novel 1,2-diarylcyclobutenes: Selective and orally active cox-2 inhibitors, Bioorg. Med. Chem. Lett. 6(22):2677-2682 (1996).
|
64 |
Synthesis and antiinflammatory/analgesic activities of 11H-dibenzo[b, e,][1,4]dioxepinacetic acids. J Med Chem. 1986 Aug;29(8):1436-41.
|
65 |
Sulfonamide derivatives of styrylheterocycles as a potent inhibitor of COX-2-mediated prostaglandin E2 production. Bioorg Med Chem Lett. 2010 Dec 1;20(23):6938-41.
|
66 |
The influence of double bond geometry in the inhibition of cyclooxygenases by sulindac derivatives. Bioorg Med Chem Lett. 2009 Jun 15;19(12):3271-4.
|
67 |
'Bridged' stilbene derivatives as selective cyclooxygenase-1 inhibitors. Bioorg Med Chem. 2007 Sep 15;15(18):6109-18.
|
68 |
Dinitroglyceryl and diazen-1-ium-1,2-diolated nitric oxide donor ester prodrugs of aspirin, indomethacin and ibuprofen: synthesis, biological evalu... Bioorg Med Chem Lett. 2009 Jun 1;19(11):3014-8.
|
69 |
Inhibitory activity of prostaglandin E2 production by the synthetic 2'-hydroxychalcone analogues: Synthesis and SAR study. Bioorg Med Chem Lett. 2009 Mar 15;19(6):1650-3.
|
70 |
Synthesis, anti-inflammatory activity, and in vitro antitumor effect of a novel class of cyclooxygenase inhibitors: 4-(aryloyl)phenyl methyl sulfones. J Med Chem. 2010 Sep 23;53(18):6560-71.
|
71 |
Design and synthesis of 1,3-diarylurea derivatives as selective cyclooxygenase (COX-2) inhibitors. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1336-9.
|
72 |
Synthesis and cyclooxygenase inhibitory activities of linear 1-(methanesulfonylphenyl or benzenesulfonamido)-2-(pyridyl)acetylene regioisomers. Bioorg Med Chem. 2008 Feb 15;16(4):1948-56.
|
73 |
Design and synthesis of ten biphenyl-neolignan derivatives and their in vitro inhibitory potency against cyclooxygenase-1/2 activity and 5-lipoxyge... Bioorg Med Chem. 2009 Jul 1;17(13):4459-65.
|
74 |
Selective cyclooxygenase-2 inhibitors from Calophyllum membranaceum. J Nat Prod. 2005 Oct;68(10):1514-8.
|
75 |
Molecular determinants for the selective inhibition of cyclooxygenase-2 by lumiracoxib. J Biol Chem. 2007 Jun 1;282(22):16379-90.
|
76 |
Indazolinones, a new series of redox-active 5-lipoxygenase inhibitors with built-in selectivity and oral activity. J Med Chem. 1991 Mar;34(3):1028-36.
|
77 |
Design, synthesis and biological evaluation of new 2,3-diarylquinoline derivatives as selective cyclooxygenase-2 inhibitors. Bioorg Med Chem. 2010 Feb;18(3):1029-33.
|
78 |
Synthesis and biological activity of new anti-inflammatory compounds containing the 1,4-benzodioxine and/or pyrrole system. Bioorg Med Chem. 2007 Jul 15;15(14):4876-90.
|
79 |
Nitrogen-containing phorbol esters from Croton ciliatoglandulifer and their effects on cyclooxygenases-1 and -2. J Nat Prod. 2006 Jun;69(6):887-90.
|
80 |
Synthesis and biological evaluation of 1,3-diphenylprop-2-yn-1-ones as dual inhibitors of cyclooxygenases and lipoxygenases. Bioorg Med Chem Lett. 2005 Nov 1;15(21):4842-5.
|
81 |
Investigations concerning the COX/5-LOX inhibiting and hydroxyl radical scavenging potencies of novel 4,5-diaryl isoselenazoles. Eur J Med Chem. 2008 Jun;43(6):1152-9.
|
82 |
Diaryl-dithiolanes and -isothiazoles: COX-1/COX-2 and 5-LOX-inhibitory, *OH scavenging and anti-adhesive activities. Bioorg Med Chem. 2009 Jan 15;17(2):558-68.
|
83 |
Selective COX-2 inhibitors. Part 1: synthesis and biological evaluation of phenylazobenzenesulfonamides. Bioorg Med Chem Lett. 2006 Sep 1;16(17):4440-3.
|
84 |
Selective COX-2 inhibitors. Part 2: synthesis and biological evaluation of 4-benzylideneamino- and 4-phenyliminomethyl-benzenesulfonamides. Bioorg Med Chem. 2008 Mar 1;16(5):2697-706.
|
85 |
Analgesic agents without gastric damage: design and synthesis of structurally simple benzenesulfonanilide-type cyclooxygenase-1-selective inhibitors. Bioorg Med Chem. 2007 Jan 15;15(2):1014-21.
|
86 |
1-imidazolyl(alkyl)-substituted di- and tetrahydroquinolines and analogues: syntheses and evaluation of dual inhibitors of thromboxane A(2) synthas... J Med Chem. 2000 May 4;43(9):1841-51.
|
87 |
Novel synthesis of 3,4-diarylisoxazole analogues of valdecoxib: reversal cyclooxygenase-2 selectivity by sulfonamide group removal. J Med Chem. 2004 Sep 23;47(20):4881-90.
|
88 |
Synthesis and biological evaluation of new 4-carboxyl quinoline derivatives as cyclooxygenase-2 inhibitors. Bioorg Med Chem. 2009 Jul 15;17(14):5312-7.
|
89 |
Differential effects of a series of hydroxamic acid derivatives on 5-lipoxygenase and cyclooxygenase from neutrophils and 12-lipoxygenase from plat... J Med Chem. 1989 Aug;32(8):1836-42.
|
90 |
Synthesis of biflavones having a 6-O-7'' linkage and effects on cyclooxygenase-2 and inducible nitric oxide synthase. Bioorg Med Chem Lett. 2009 Jan 1;19(1):74-6.
|
91 |
Cyclooxygenase (COX)-1 and -2 inhibitory labdane diterpenes from Crassocephalum mannii. J Nat Prod. 2008 Jun;71(6):1070-3.
|
92 |
How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
|
93 |
Cyclooxygenase-2, a colorectal cancer nonsteroidal anti-inflammatory drug target, is regulated by c-MYB. Cancer Res. 2000 Apr 1;60(7):1805-9.
|
94 |
Triterpene saponins from clematis mandshurica. J Nat Prod. 2006 Nov;69(11):1591-5.
|
95 |
URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1376).
|
96 |
Inhibition of cyclooxygenase-2 improves cardiac function in myocardial infarction. Biochem Biophys Res Commun. 2000 Jul 5;273(2):772-5.
|
97 |
SAR in the alkoxy lactone series: the discovery of DFP, a potent and orally active COX-2 inhibitor. Bioorg Med Chem Lett. 1999 Aug 2;9(15):2207-12.
|
98 |
Properties and synthesis of 2-{2-fluoro (or bromo)-4-[(2-oxocyclopentyl)methyl]phenyl}propanoic acid: nonsteroidal anti-inflammatory drugs with low... J Med Chem. 2010 Nov 11;53(21):7879-82.
|
99 |
Identification of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidinyl] amines and ethers as potent and selective cyclooxygenase-2 inhib... Bioorg Med Chem Lett. 2009 Aug 1;19(15):4504-8.
|
100 |
The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
|
101 |
From indomethacin to a selective COX-2 inhibitor: Development of indolalkanoic acids as potent and selective cyclooxygenase-2 inhibitors, Bioorg. Med. Chem. Lett. 6(6):725-730 (1996).
|
102 |
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 ... Bioorg Med Chem. 2010 Jan 15;18(2):597-604.
|
103 |
Inhibition of cell cycle oscillation of DNA replication by a selective inhibitor of the cdc2 kinase family, butyrolactone I, in Xenopus egg extracts. Biochem Biophys Res Commun. 1994 Jan 28;198(2):536-45.
|
104 |
New analgesics synthetically derived from the paracetamol metabolite N-(4-hydroxyphenyl)-(5Z,8Z,11Z,14Z)-icosatetra-5,8,11,14-enamide. J Med Chem. 2008 Dec 25;51(24):7800-5.
|
105 |
Pyridine analogues of nimesulide: design, synthesis, and in vitro and in vivo pharmacological evaluation as promising cyclooxygenase 1 and 2 inhibi... J Med Chem. 2009 Oct 8;52(19):5864-71.
|
106 |
Design, synthesis, and pharmacological evaluation of pyridinic analogues of nimesulide as cyclooxygenase-2 selective inhibitors. J Med Chem. 2004 Dec 30;47(27):6749-59.
|
107 |
COX, LOX and platelet aggregation inhibitory properties of Lauraceae neolignans. Bioorg Med Chem Lett. 2009 Dec 15;19(24):6922-5.
|
108 |
The cyclooxygenase inhibitor flurbiprofen reduces radiation-induced angiogenic growth factor secretion of squamous cell carcinoma cell lines. Ann N Y Acad Sci. 2004 Dec;1030:37-42.
|
109 |
Structure-based design, synthesis, and biological evaluation of indomethacin derivatives as cyclooxygenase-2 inhibiting nitric oxide donors. J Med Chem. 2007 Dec 13;50(25):6367-82.
|
110 |
A selective inhibitor of p38 MAP kinase, SB202190, induced apoptotic cell death of a lipopolysaccharide-treated macrophage-like cell line, J774.1. Biochim Biophys Acta. 2000 Oct 18;1502(2):207-23.
|
111 |
PAC 10649 Pacific licensing offer, Worldwide excluding South Korea. R & D Focus Drug News. September 22, 2003.
|
112 |
Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43.
|
113 |
Diazen-1-ium-1,2-diolated nitric oxide donor ester prodrugs of 5-(4-hydroxymethylphenyl)-1-(4-aminosulfonylphenyl)-3-trifluoromethyl-1H-pyrazole an... Bioorg Med Chem. 2008 Nov 15;16(22):9694-8.
|
114 |
Selective synthesis and biological evaluation of sulfate-conjugated resveratrol metabolites. J Med Chem. 2010 Jul 8;53(13):5033-43.
|
115 |
SB-239063, a potent and selective inhibitor of p38 map kinase: preclinical pharmacokinetics and species-specific reversible isomerization. Pharm Res. 2001 Sep;18(9):1336-44.
|
116 |
In silico search for multi-target anti-inflammatories in Chinese herbs and formulas. Bioorg Med Chem. 2010 Mar 15;18(6):2204-2218.
|
117 |
US patent application no. 6,274,627, Conjugates of dithiocarbamate disulfides with pharmacologically active agents and uses therefor.
|
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