Diaryloxazole and Diarylthiazolealkanoic Acids: Two Novel Series of Non-steroidal Anti-inflammatory Agents

@article{Brown1968DiaryloxazoleAD,
  title={Diaryloxazole and Diarylthiazolealkanoic Acids: Two Novel Series of Non-steroidal Anti-inflammatory Agents},
  author={Kevan Brown and John Frederick Cavalla and D Green and A. B. Wilson},
  journal={Nature},
  year={1968},
  volume={219},
  pages={164-164}
}
SINCE the reports of the anti-inflammatory activity of indomethacin (1-p-chlorobenzoyl-5-methoxy-2-methyl-indol-3-ylacetic acid)1 and ibufenac (p-isobutylphenylacetic acid)2, there has been much interest in the pharmacological properties of aryl and heteroarylalkanoic acids. This paper describes the anti-inflammatory activity found in two series of new alkanoic acids, namely the 2,4-di-phenylthiazol-5-ylacetic acids (I) and the β-(4,5-diphenyl-oxazol-2-yl) propionic acids (II). The thiazoles (I… Expand
Synthesis of 5-aryl-2-oxazolepropionic acids and analogs. Antiinflammatory agents
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The synthesis and biological properties of a new and potent series of anti-inflammatory agents which manifest similar structural features of different groups of non-steroidal ariti- inflammatory agents are reported. Expand
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The oxazole, oxaprozin has a spectrum of activity in various in vivo and in vitro, chronic and acute inflammatory models in 3 species indicating that it belongs to the general class of non-steroidalExpand
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Perspectives in nonsteroidal anti-inflammatory agents.
  • T. Shen
  • Chemistry, Medicine
  • Angewandte Chemie
  • 1972
TLDR
Competitive binding and antagonistic interactions between nonsteroidal drugs, particularly salicylate, were observed in vitro and in vivo. Expand
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References

SHOWING 1-7 OF 7 REFERENCES
Indomethacin in Rheumatic Diseases
TLDR
Experiences with Indomethacin over the last year in the treatment of rheumatoid arthritis and other conditions are reported. Expand
Phenylbutazone (butazolidin) in rheumatoid arthritis and gout.
Phenylbutazone (butazolidin®) is one of a group of pyrazole derivatives developed by the chemists of the J. R. Geigy Co., of Basel, Switzerland, in an attempt to find compounds with pharmacologieExpand
Some Biological Properties of ‘Ibufenac’, a New Anti-rheumatic Drug
TLDR
The properties of ‘Ibufenac’, which Chalmers and Duthie have recently shown to be effective in the treatment of rheumatoid arthritis, are described. Expand
Monks Wood Experimental Station