Anti-inflammatory and other pharmacodynamic properties of five members of the 4-aryl-1-isopropyl-2(1H)-quinazolinone series.
A series of five 4-aryl-1-isopropyl-2(1H)-quinazolinone analogs were examined for their relative activities regarding analgesia, suppression of inflammation and pyresis, and associated phenomena. Two of these, proquazone (SaH 43-715, Biarsan, Biarison) and fluproquazone (SaH 46-790), are clinically effective anti-inflammatory and analgesic agents. Acetylsalicylic acid (ASA) and phenylbutazone were included for reference as first and second generation nonsteroidal anti-inflammatory drugs (NSAID), respectively. In general, substitutions in these five quinazolinone analogs produced noticeable changes in potency in several activities but changes of lesser degrees in others. Compared to ASA and phenylbutazone the quinazolinones exhibited better analgesic and related activities.
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology* / Q000633:toxicity; D000894:Anti-Inflammatory Agents, Non-Steroidal; D001169:Arthritis, Experimental / Q000188:drug therapy; D001786:Blood Glucose / Q000378:metabolism; D001993:Bronchodilator Agents; D002490:Central Nervous System / Q000187:drug effects; D055598:Chemical Phenomena; D002621:Chemistry; D002645:Chickens; D005334:Fever / Q000188:drug therapy; D006168:Guinea Pigs; D006439:Hemodynamics / Q000187:drug effects; D007004:Hypoglycemic Agents; D008297:Male; D051379:Mice; D011799:Quinazolines / Q000494:pharmacology*; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains; D013276:Stomach Ulcer / Q000139:chemically induced; D013997:Time Factors
D000893:Anti-Inflammatory Agents; D000894:Anti-Inflammatory Agents, Non-Steroidal; D001786:Blood Glucose; D001993:Bronchodilator Agents; D007004:Hypoglycemic Agents; D011799:Quinazolines