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

  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},
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… 

Synthesis of 5-aryl-2-oxazolepropionic acids and analogs. Antiinflammatory agents

Condensation of 2-bromoacetophenones with sodium succinimide gave N-phenacylsuccinimides (1) which were opened with sodium hydroxide to N-phenacylsuccinamic acids (2). The latter were cyclized to

Synthesis of some 5,6-diaryl-1,2,4-triazine derivatives and investigation of their cyclooxygenase (COX) inhibitory activity

Abstract Within this study, 20 2-[(5,6-diaryl-1,2,4-triazin-3-yl)thio]-N-(benzo/thiazol-2-yl)acetamide derivatives (4a-4t) were synthesized and COX inhibitory activities of the compounds were

Dioxoisoquinoline-4-carboxanilides—A New Class of Non-steroidal Anti-inflammatory Agents

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.

Design, synthesis, and in-vivo evaluation of 4,5-diaryloxazole as novel nonsteroidal anti-inflammatory drug.

After the aminosulfonyl group was introduced into the benzene ring of oxaprozin, its analgesic and anti-inflammatory activities remained unchanged, and it reduced the number of gastric lesions, which provided a feasible method for further structure modification and optimization of oxAProzin.

Anti-inflammatory properties of 4,5-diphenyl-2-oxazolepropionic acid (oxaprozin)

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-steroidal

Synthesis and properties of 4-phosphorylated derivatives of 5-hydroxyalkylamino-1,3-oxazoles

Reactions of derivatives of diethyl 1-acylamino-2,2,2-trichloroethylphosphonates with different pharmacophore aminoalkanols afforded new 5-hydroxyalkylamino-1,3-oxazole derivatives. The latter are

Structural diversity of selective COX-2 inhibitors

These bioactive lipids mediate numerous physiological and pathophysiological effects, including pain, fever, inflammation, hemostasis, and regulation of renal function and maintenance of mucosal integrity in the stomach.



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