Search results for "Phenylbutazone"

Phenylamides of 1-Phenyl (or Methyl)-5-benzamidopyrazole-4-carboxylic Acid as Vratizolin Analogs with Analgesic and Antiinflammatory Activities

2001

A number of phenylamides of 5-benzamidopyrazole-4-carboxylic acid were prepared in 50-80 % yields from 1-phenyl (or methyl) 6-phenylpyrazolo[3,4-d]1,3-oxazin-4(1H)-ones and aniline derivatives. All the compounds were tested for their analgesic and antiinflammatory activities, as well as for their ulcerogenic potential and acute toxicity. Some derivatives, when compared to phenylbutazone, proved more active in the tests for analgesie and antiexudative activities, but less active in the carrageenin paw oedema test. The compounds proved to posses marginal or no ulcerogenic effect, as well as low systemic toxicity.

Zur Wirkung von Butazolidin auf Glutamins�ure-dehydrogenase und ?-Ketoglutarat-oxydase

1957

Glutamic dehydrogenase of rat liver mitochondria is inhibited by phenylbutazone at a final concentration of 2,5 mg-% (0,81 · 10−4 M). However, glutamic dehydrogenase in heart muscle homogenate and the cristalline enzyme from liver are not inhibited by phenylbutazone up to 10 mg-% (3,24 · 10−4 M), but they are inhibited by a metabolite arising during incubation of liver mitochondria with phenylbutazone.

ChemInform Abstract: Synthesis and Pharmacological Evaluation of 1-Methyl-5- [substituted-4(3H)-oxo-1,2,3-benzotriazin-3-yl]-1H-pyrazole-4-acetic Aci…

2010

Abstract Several new 1-methyl-5-[substituted-4-oxo-1,2,3-benzotriazin-3-yl]-1H-pyrazole-4-acetic acids and their ethyl ester derivatives were prepared. The compounds were tested for analgesic and antiinflammatory activities, acute toxicity, ulcerogenic effect, and as in vitro inhibitors of 3α-hydroxysteroid dehydrogenase (3α-HSD), since it is claimed that the inhibition of such an enzyme predicts in vivo antiinflammatory activity. Some compounds were more active than phenylbutazone in the phenylbenzoquinone and acetic acid peritonitis tests, and equiactive to the same drug in the carrageenin paw edema test. All the compounds inhibited the 3α-HSD, but no correlation was observed with the paw…

Reaction of 4-acylaminomethylpyridine N-oxides with phenylbutazone in the presence of acetic anhydride

1987