6533b85ffe1ef96bd12c1cb1

RESEARCH PRODUCT

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

Nunzio Guido ManganoRaffa DemetrioFabiana PlesciaAntonina CarusoVincenza Maria Catena CutuliBenedetta MaggioGiuseppe Daidone

subject

Malemedicine.drug_classCarboxylic acidAnalgesicDrug Evaluation PreclinicalPharmaceutical ScienceCarboxamideChemical synthesisRats Sprague-DawleyMiceStructure-Activity Relationshipchemistry.chemical_compoundAnilineDrug DiscoveryPhenylbutazonemedicineAnimalsOrganic chemistrychemistry.chemical_classificationAnalgesicsDose-Response Relationship DrugAcute toxicityRatsThiazoleschemistryBenzamidesToxicityPyrazolesInflammation Mediatorsmedicine.drug

description

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.

https://doi.org/10.1002/1521-4184(200105)334:5<153::aid-ardp153>3.0.co;2-7