6533b7dbfe1ef96bd126fdf5
RESEARCH PRODUCT
ChemInform Abstract: Synthesis and Pharmacological Evaluation of 1-Methyl-5- [substituted-4(3H)-oxo-1,2,3-benzotriazin-3-yl]-1H-pyrazole-4-acetic Acid Derivatives.
Domenico SchillaciM. Amico-roxasBenedetta MaggioGiuseppe DaidoneOnofrio MigliaraDemetrio RaffaVincenza Maria Catena CutuliSalvatore PlesciaAntonina Carusosubject
chemistry.chemical_classificationChemistryDehydrogenaseGeneral MedicinePyrazoleMedicinal chemistryAcute toxicityIn vitroAcetic acidchemistry.chemical_compoundEnzymeIn vivoPhenylbutazonemedicinemedicine.drugdescription
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 edema inhibition values. The compounds proved to possess marginal or no ulcerogenic effect, as well as low systemic toxicity.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2010-06-19 | ChemInform |