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Pharmacological studies on quaternized 4(3H)-quinazolinones
S Buyuktimkin1, A C Ekinci, N Buyuktimkin
1Faculty of Pharmacy, University of Istanbul, Beyazit, Turkey.
Journal of Pharmaceutical Sciences
|November 1, 1992
Summary
New quinazolinone derivatives show promising anticonvulsant and analgesic effects, with compound 2 exhibiting activity comparable to methaqualone and aspirin. These compounds did not display antimicrobial or muscle relaxant properties.
Area of Science:
- Medicinal Chemistry
- Pharmacology
Background:
- Quinazolinone derivatives are known for diverse pharmacological activities.
- Exploring novel chemical structures is crucial for drug discovery.
Purpose of the Study:
- To synthesize and evaluate the pharmacological properties of five novel quinazolinone derivatives.
- To investigate their potential as anticonvulsant, analgesic, muscle relaxant, and antimicrobial agents.
Main Methods:
- Synthesis of five quinazolinone chloride derivatives.
- Assessment of locomotor activity inhibition and anticonvulsant activity.
- Evaluation of analgesic effects using hot-plate and Koster tests.
- Screening for antimicrobial and muscle relaxant properties.
Main Results:
- Compound 2 demonstrated significant locomotor activity-inhibiting and anticonvulsant properties, comparable to methaqualone.
- Compounds 2 and 3 exhibited analgesic activity similar to aspirin in the hot-plate test, with compound 2 showing superior efficacy in the Koster test.
- No antimicrobial or muscle relaxant activities were observed for any of the tested compounds.
- Higher lipophilicity correlated with increased activity in the most effective compounds.
Conclusions:
- Novel quinazolinone derivatives, particularly compound 2, possess notable anticonvulsant and analgesic potential.
- Lipophilicity appears to be a key factor influencing the observed pharmacological activities.
- Further research into these compounds could lead to the development of new therapeutic agents.