6533b86dfe1ef96bd12c9677
RESEARCH PRODUCT
Synthesis and pharmacological evaluation of 1-methyl-5- [substituted-4(3H)-oxo-1,2,3-benzotriazin-3-yl]-1H-pyrazole-4-acetic acid derivatives
M. Amico-roxasOnofrio MigliaraSalvatore PlesciaBenedetta MaggioVincenza Maria Catena CutuliDomenico SchillaciRaffa DemetrioGiuseppe DaidoneAntonina Carusosubject
Male3-Hydroxysteroid DehydrogenasesStereochemistryAnti-Inflammatory AgentsPharmaceutical SciencePyrazoleChemical synthesisMicechemistry.chemical_compoundAcetic acidIn vivoDrug DiscoveryPhenylbutazonemedicineAnimalsEnzyme InhibitorsAnalgesicsbiology3-alpha-Hydroxysteroid Dehydrogenase (B-Specific)Acute toxicityRatschemistryEnzyme inhibitorToxicitybiology.proteinPyrazolesmedicine.drugdescription
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 3 alpha-hydroxysteroid dehydrogenase (3 alpha-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 3 alpha-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 |
|---|---|---|---|---|
| 1998-05-01 | Il Farmaco |