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)-...

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Bibliographic Details
Published in:Journal of pharmaceutical sciences 1992-11, Vol.81 (11), p.1092-1094
Main Authors: Buyuktimkin, S., Ekinci, A.C., Buyuktimkin, N., Otuk, G.
Format: Article
Language:English
Subjects:
Analgesics
Animals
Anti-Infective Agents - chemistry
Anti-Infective Agents - pharmacology
Anticonvulsants - chemistry
Anticonvulsants - pharmacology
Biological and medical sciences
Hypnotics and Sedatives - pharmacology
Medical sciences
Mice
Muscle Relaxation - drug effects
Neuropharmacology
Pharmacology. Drug treatments
Quinazolines - chemistry
Quinazolines - pharmacology
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Summary: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)-quinazolinone 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.
ISSN:0022-3549
1520-6017
DOI:10.1002/jps.2600811110