0000000000039757

AUTHOR

Nunzio Guido Mangano

showing 4 related works from this author

Synthesis and Pharmacological Activities of Novel 3-(Isoxazol-3-yl)-quinazolin-4(3H)-one Derivatives

1999

Several new 3-(isoxazol-3-yl)-quinazolin-4(3H)-one derivatives were synthesized and tested for their analgesic and antiinflammatory activities, as well as for their acute toxicity and ulcerogenic effect. A few compounds were as active as phenylbutazone in the writhing and acetic acid peritonitis tests. They had a very low ulcerogenic effect.

MaleStereochemistryAnalgesicAnti-Inflammatory AgentsPharmaceutical ScienceChemical synthesisRats Sprague-DawleyMiceStructure-Activity Relationshipchemistry.chemical_compoundAcetic acidDrug DiscoveryPhenylbutazonemedicineAnimalsStomach UlcerNuclear Magnetic Resonance BiomolecularAnalgesicsBehavior AnimalBicyclic moleculeAcute toxicityRatschemistryToxicityQuinazolinesLactammedicine.drugArchiv der Pharmazie
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Synthesis and pharmacological study of ethyl 1-methyl-5-(substituted 3,4-dihydro-4-oxoquinazolin-3-yl)-1H-pyrazole-4-acetates

2001

Several new ethyl 1-methyl-5-(substituted 3,4-dihydro-4-oxoquinazolin-3-yl)-1H-pyrazole-4-acetates 2, substituted at 2 and, alternatively at, 6, 7 or 8 positions of the quinazolinone nucleus, were synthesised. The compounds were screened for their analgesic and antiinflammatory activities, acute toxicity and ulcerogenic effect. Substitution in the benzene moiety of the quinazolinone ring did not show any advantage for the analgesic activity, whereas it improved in some cases the antiinflammatory activity. Some compounds showed appreciable antiinflammatory activity and, at the same time, very low ulcerogenic index.

MaleMagnetic Resonance SpectroscopySpectrophotometry InfraredStereochemistryAnalgesicAnti-Inflammatory AgentsPeritonitisPyrazoleChemical synthesisLethal Dose 50Rats Sprague-DawleyMicechemistry.chemical_compoundDrug DiscoveryBenzoquinonesAnimalsEdemaMoietyStomach UlcerQuinazolinonePharmacologyAnalgesicsBicyclic moleculeOrganic ChemistryGeneral MedicineAcute toxicityRatschemistryQuinazolinesLactamPyrazolesEuropean Journal of Medicinal Chemistry
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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.

Malemedicine.drug_classCarboxylic acidAnalgesicDrug Evaluation PreclinicalPharmaceutical ScienceCarboxamideChemical synthesisRats Sprague-DawleyMiceStructure-Activity Relationshipchemistry.chemical_compoundAnilineDrug DiscoveryPhenylbutazonemedicineAnimalsOrganic chemistrychemistry.chemical_classificationAnalgesicsDose-Response Relationship DrugAcute toxicityRatsThiazoleschemistryBenzamidesToxicityPyrazolesInflammation Mediatorsmedicine.drugArchiv der Pharmazie
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ChemInform Abstract: Synthesis and Pharmacological Activities of Novel 3-(Isoxazol-3-yl)-quinazolin-4(3H)-one Derivatives.

2010

Several new 3-(isoxazol-3-yl)-quinazolin-4(3H)-one derivatives were synthesized and tested for their analgesic and antiinflammatory activities, as well as for their acute toxicity and ulcerogenic effect. A few compounds were as active as phenylbutazone in the writhing and acetic acid peritonitis tests. They had a very low ulcerogenic effect.

Acetic acidchemistry.chemical_compoundChemistryAnalgesicmedicinePhenylbutazonePeritonitisGeneral MedicinePharmacologymedicine.diseaseAcute toxicitymedicine.drugChemInform
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