Synthesis and pharmacological study of ethyl 1-methyl-5-(substituted 3,4-dihydro-4-oxoquinazolin-3-yl)-1H-pyrazole-4-acetates
Autor: | Nunzio Guido Mangano, Giuseppe Daidone, Vincenza Maria Catena Cutuli, Luca Mantione, Antonina Caruso, Benedetta Maggio, Demetrio Raffa, Salvatore Plescia |
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Rok vydání: | 2001 |
Předmět: |
Male
Magnetic Resonance Spectroscopy Spectrophotometry Infrared Stereochemistry Analgesic Anti-Inflammatory Agents Peritonitis Pyrazole Chemical synthesis Lethal Dose 50 Rats Sprague-Dawley Mice chemistry.chemical_compound Drug Discovery Benzoquinones Animals Edema Moiety Stomach Ulcer Quinazolinone Pharmacology Analgesics Bicyclic molecule Organic Chemistry General Medicine Acute toxicity Rats chemistry Quinazolines Lactam Pyrazoles |
Zdroj: | European Journal of Medicinal Chemistry. 36:737-742 |
ISSN: | 0223-5234 |
Popis: | 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. |
Databáze: | OpenAIRE |
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