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… 

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References

SHOWING 1-7 OF 7 REFERENCES

Indomethacin in Rheumatic Diseases

Experiences with Indomethacin over the last year in the treatment of rheumatoid arthritis and other conditions are reported.

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 pharmacologie

Some Biological Properties of ‘Ibufenac’, a New Anti-rheumatic Drug

The properties of ‘Ibufenac’, which Chalmers and Duthie have recently shown to be effective in the treatment of rheumatoid arthritis, are described.

Monks Wood Experimental Station