Non-steroidal anti-inflammatory agents: novel pyrazolyl-, 1,2-oxazolyl-, and 1,3-diazinyl derivatives of 4(3H)-quinazolinones.
Four novel series of 4(3H)-quinazolinone derivatives have been prepared by cyclization of the key intermediates 3-aryl-2-(3-aryl-3-oxopropenyl)-4-(3H)-quinazolinones with different reagents: 3-aryl-1-iminocarbamoyl-1H-pyrazol-5-yl)-4(3H)-quinazolines, 3-aryl-2-(3-aryl-1-thiocarbamoyl-1H-pyrazol-5-yl)-4(3H)-quinazolines, 3-aryl-2-(3-aryl-4,5-dihydro-1,2-oxazol-5-yl)-4(3H)-quinazolinones , and 3-aryl-2-(4-aryl-2-thioxo-1,2,5,6-tetrahydro-1,3-diazin-6-yl )-4(3H)- quinazolinones. The antiinflammatory activity of representatives of these compounds is comparable to or higher than that of proquazone.
Khalil
M A
MA
Pharmaceutical Chemistry Department, Faculty of Pharmacy, University of Alexandria, Egypt.
Soliman
R
R
Farghaly
A M
AM
Bekhit
A A
AA
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000494:pharmacology; D006099:Granuloma / Q000139:chemically induced / Q000517:prevention & control; D008297:Male; D010080:Oxazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley
D000894:Anti-Inflammatory Agents, Non-Steroidal; D010080:Oxazoles; D011720:Pyrazoles; D011799:Quinazolines