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

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 tox...

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Published in:European journal of medicinal chemistry 2001-09, Vol.36 (9), p.737-742
Main Authors: MAGGIO, Benedetta, DAIDONE, Giuseppe, RAFFA, Demetrio, PLESCIA, Salvatore, MANTIONE, Luca, CATENA CUTULI, Vincenza Maria, MANGANO, Nunzio Guido, CARUSO, Antonina
Format: Article
Language:English
Subjects:
Analgesics
Analgesics - chemical synthesis
Analgesics - pharmacology
Analgesics - toxicity
Animals
Anti-Inflammatory Agents - chemical synthesis
Anti-Inflammatory Agents - pharmacology
Anti-Inflammatory Agents - toxicity
Benzoquinones - pharmacology
Biological and medical sciences
Edema - chemically induced
Lethal Dose 50
Magnetic Resonance Spectroscopy
Male
Medical sciences
Mice
Neuropharmacology
Peritonitis
Pharmacology. Drug treatments
Pyrazoles - chemical synthesis
Pyrazoles - pharmacology
Pyrazoles - toxicity
Quinazolines - chemical synthesis
Quinazolines - pharmacology
Quinazolines - toxicity
Rats
Rats, Sprague-Dawley
Spectrophotometry, Infrared
Stomach Ulcer - chemically induced
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Summary: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.
ISSN:0223-5234
1768-3254
DOI:10.1016/S0223-5234(01)01259-4