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… Expand
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 toExpand
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. Expand
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. Expand
Relationship between antiinflamatory and antiproteolytic properties of substituted oxothiazolylacetic acids.
Six 2-substituted imino-3(3-diethylaminopropyl)-4-oxothiazol-5-ylacetic acids were synthesized, characterized and evaluated for their anti inflammatory and antiproteolytic properties and protection against carrageenin-induced edema in rats. Expand
Potent antiinflammatory 3-thiazole-4(5)-acetic acids of 1,2-benzisothiazole
Abstract A number of 1,2-benzisothiazole derivatives, having 2-thiazolyl-4(5)-acetic acid moiety attached to position-3 of 1,2-benzisothiazole nucleus, were prepared and evaluated as antiinflammatoryExpand
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-steroidalExpand
Design and synthesis of some thiazolotriazolyl esters as anti-inflammatory and analgesic agents
In order to develop potent analgesic/anti-inflammatory compounds with reduced ulcerogenic risk, a series of thiazolotriazolyl-carboxylic and acetic acid esters were synthesized and characterized byExpand
Synthesis and evaluation of some amino acid conjugates of pirprofen
Abstract Amino acid conjugates of suprofen were synthesized by coupling the carboxylic group (as acid chloride) of suprofen and various amino acid methyl ester hydrochlorides. The structures of theExpand
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 areExpand
Perspectives in nonsteroidal anti-inflammatory agents.
  • T. Shen
  • Chemistry, Medicine
  • Angewandte Chemie
  • 1972
Competitive binding and antagonistic interactions between nonsteroidal drugs, particularly salicylate, were observed in vitro and in vivo. Expand


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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
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Monks Wood Experimental Station