Journal ArticleDOI
1,3-Diarylcycloalkanopyrazoles and diphenyl hydrazides as selective inhibitors of cyclooxygenase-2.
Zhihua Sui,Jihua Guan,Michael Paul Ferro,Kathy McCoy,Michael P. Wachter,William V. Murray,Monica Singer,Michele Steber,Dave M. Ritchie,Dennis C. Argentieri +9 more
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TLDR
Novel 1,3-diarylcycloalkanopyrazoles 1, and diphenyl hydrazides 2 were identified as selective inhibitors of cyclooxygenase-2 and SAR of both phenyl rings in 1 and 2, and the aliphatic ring in 1 will be discussed.About:
This article is published in Bioorganic & Medicinal Chemistry Letters.The article was published on 2000-03-20. It has received 72 citations till now. The article focuses on the topics: Pyrazole & Bicyclic molecule.read more
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Visible-Light Photocatalysis: Does It Make a Difference in Organic Synthesis?
TL;DR: This Review compares classical and photocatalytic procedures for selected classes of reactions and highlights their advantages and limitations.
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From 2000 to mid-2010: a fruitful decade for the synthesis of pyrazoles.
Journal ArticleDOI
Photokatalyse mit sichtbarem Licht: Welche Bedeutung hat sie für die organische Synthese?
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Recent Advances in the Synthesis of Pyrazoles. A Review
TL;DR: A five-membered, two-nitrogen-containing heterocycle ring is widely found as the core structure in a large variety of compounds that possess important agrochemical and pharmacological properties as mentioned in this paper.
Journal ArticleDOI
Progress in COX-2 Inhibitors: A Journey So Far
TL;DR: This review highlights the various structural classes of selective COX-2 inhibitors developed during past seven years with special emphasis on diaryl-hetero/carbo-cyclic class of compounds.
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Journal ArticleDOI
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]benze nesulfonamide (SC-58635, celecoxib).
T. D. Penning,John J. Talley,Bertenshaw,Jeffery S. Carter,P. W. Collins,Stephen H. Docter,Matthew J. Graneto,Len F. Lee,James W. Malecha,Julie M. Miyashiro,Roland S. Rogers,D. J. Rogier,Stella S. Yu,AndersonGD,E. G. Burton,J. N. Cogburn,Susan A. Gregory,Carol M. Koboldt,W E Perkins,Karen Seibert,A. W. Veenhuizen,Yan Y. Zhang,P. C. Isakson +22 more
TL;DR: 1i (4-[5-(4-methylphenyl)-3-(trifluoromethyl)- H-pyrazol-1-yl]benzenesulfonamide, SC-58635, celecoxib), which is currently in phase III clinical trials for the treatment of rheumatoid arthritis and osteoarthritis, is identified.
Journal Article
International Union of Pharmacology classification of prostanoid receptors: properties, distribution, and structure of the receptors and their subtypes.
Journal ArticleDOI
Selectivity of nonsteroidal antiinflammatory drugs as inhibitors of constitutive and inducible cyclooxygenase
TL;DR: BF 389, an experimental drug currently being tested in humans, was the most potent and most selective inhibitor of COX-2 in intact cells, indicating there are clear pharmacological differences between the two enzymes.
Journal ArticleDOI
Pharmacological and biochemical demonstration of the role of cyclooxygenase 2 in inflammation and pain.
Karen Seibert,Yan Zhang,Kathleen M. Leahy,Scott D. Hauser,Jaime L. Masferrer,William Perkins,Len F. Lee,Peter C. Isakson +7 more
TL;DR: In an animal model of acute inflammation, a selective inhibitor of COX-2 inhibited edema at the inflammatory site and was analgesic but had no effect on PG production in the stomach and did not cause gastric toxicity.
Journal ArticleDOI
Expression of mRNA for cyclooxygenase‐1 and cyclooxygenase‐2 in human tissues
TL;DR: In this article, the authors quantified the expression of COX-1 and COX2 mRNA in human tissues including lung, uterus, testis, brain, pancreas, kidney, liver, thymus, prostate, mammary gland, stomach and small intestine.
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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]benze nesulfonamide (SC-58635, celecoxib).
T. D. Penning,John J. Talley,Bertenshaw,Jeffery S. Carter,P. W. Collins,Stephen H. Docter,Matthew J. Graneto,Len F. Lee,James W. Malecha,Julie M. Miyashiro,Roland S. Rogers,D. J. Rogier,Stella S. Yu,AndersonGD,E. G. Burton,J. N. Cogburn,Susan A. Gregory,Carol M. Koboldt,W E Perkins,Karen Seibert,A. W. Veenhuizen,Yan Y. Zhang,P. C. Isakson +22 more