0000000000370975

AUTHOR

M. Amico-roxas

showing 2 related works from this author

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…

chemistry.chemical_classificationChemistryDehydrogenaseGeneral MedicinePyrazoleMedicinal chemistryAcute toxicityIn vitroAcetic acidchemistry.chemical_compoundEnzymeIn vivoPhenylbutazonemedicinemedicine.drugChemInform
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Synthesis and pharmacological evaluation of 1-methyl-5- [substituted-4(3H)-oxo-1,2,3-benzotriazin-3-yl]-1H-pyrazole-4-acetic acid derivatives

1998

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 …

Male3-Hydroxysteroid DehydrogenasesStereochemistryAnti-Inflammatory AgentsPharmaceutical SciencePyrazoleChemical synthesisMicechemistry.chemical_compoundAcetic acidIn vivoDrug DiscoveryPhenylbutazonemedicineAnimalsEnzyme InhibitorsAnalgesicsbiology3-alpha-Hydroxysteroid Dehydrogenase (B-Specific)Acute toxicityRatschemistryEnzyme inhibitorToxicitybiology.proteinPyrazolesmedicine.drugIl Farmaco
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