Pharmacological studies on quaternized 4(3H)-quinazolinones.
Locomotor activity-inhibiting, anticonvulsant, muscle relaxant, analgesic, and antimicrobial properties of 2-methyl-3-pyridinium-acetylamino-4(3H)-quinazolinone chloride (1), 2-methyl-3-(4-methylpyridinium)acetylamino-4(3H)-quinazolinone chloride (2), 2-methyl-3-(4-ethylpyridinium)acetylamino-4(3H)-quinazolinone chloride (3), 2-methyl-3-(3-carboxamidopyridinium)acetylamino-4(3H)-quinazolinon e chloride (4), and 2-methyl-3-(4-carboxamidopyridinium)-acetylamino-4(3H)- quinazolinone chloride (5) were investigated. The locomotor activity-inhibiting properties and anticonvulsant activity of 2 were almost equal to those of methaqualone. The analgesic activities of 2 and 3 in the hot-plate test were equal to that of aspirin, whereas in the Koster test, the analgesic activity of 2 was higher. The compounds did not exhibit antimicrobial or muscle relaxant properties. Most active compounds had higher lipophilicity values than those of inactive compounds.
Buyuktimkin
S
S
Faculty of Pharmacy, University of Istanbul, Beyazit, Turkey.
Ekinci
A C
AC
Buyuktimkin
N
N
Otuk
G
G
D000818:Animals; D000890:Anti-Infective Agents / Q000737:chemistry / Q000494:pharmacology; D000927:Anticonvulsants / Q000737:chemistry / Q000494:pharmacology; D006993:Hypnotics and Sedatives / Q000494:pharmacology; D051379:Mice; D009126:Muscle Relaxation / Q000187:drug effects; D011799:Quinazolines / Q000737:chemistry / Q000494:pharmacology*
D000890:Anti-Infective Agents; D000927:Anticonvulsants; D006993:Hypnotics and Sedatives; D011799:Quinazolines