6533b82cfe1ef96bd128eb7f

RESEARCH PRODUCT

Synthesis and pharmacological study of ethyl 1-methyl-5-(substituted 3,4-dihydro-4-oxoquinazolin-3-yl)-1H-pyrazole-4-acetates

Nunzio Guido ManganoGiuseppe DaidoneVincenza Maria Catena CutuliLuca MantioneAntonina CarusoBenedetta MaggioDemetrio RaffaSalvatore Plescia

subject

MaleMagnetic Resonance SpectroscopySpectrophotometry InfraredStereochemistryAnalgesicAnti-Inflammatory AgentsPeritonitisPyrazoleChemical synthesisLethal Dose 50Rats Sprague-DawleyMicechemistry.chemical_compoundDrug DiscoveryBenzoquinonesAnimalsEdemaMoietyStomach UlcerQuinazolinonePharmacologyAnalgesicsBicyclic moleculeOrganic ChemistryGeneral MedicineAcute toxicityRatschemistryQuinazolinesLactamPyrazoles

description

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.

https://doi.org/10.1016/s0223-5234(01)01259-4