POSSIBLE CNS DEPRESSANT EFFECTS OF SOME NEWLY SYNTHESIZED QUINAZOLINONE DERIVATIVES | ||||
| Bulletin of Pharmaceutical Sciences Assiut University | ||||
| Article 1, Volume 13, Issue 2, December 1990, Page 137-144 PDF (368.63 K) | ||||
| DOI: 10.21608/bfsa.1990.70558 | ||||
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| Authors | ||||
| M. M. Abdel-Rahman; S. A. Mangoura; H. I. El-Bitar | ||||
| Department of Pharmacology, Faculty of Medicine, Assiut University, Assiut, Eqypt | ||||
| Abstract | ||||
| In the present investigation, five recently synthesized derivatives (designated as compounds I, II, III, IV and V) of 2,3-disubstituted 4 (3H)-quinazolinone (I) were evaluated for their CNS depressant activities in mice. In the course of this study, all compounds were suspended in a 5% suspension of gum acacia in water and were injected i.p. with the test compound in a dose level of 60 mg/kg. All tested compounds were found to decrease spontaneous locomotor activity of mice. Only compound IV was found to potentiate pentobarbitone induced hypnosis. Regarding the effect on the skeletal muscle activity, quinazolinone derivatives II and III led to motor incoordination in 40% of mice. Out of the five tested compounds, compounds I, II and IV resulted in an increase in the mean survival time of strychnine-injected mice and a greater protection against death in these animals. However, the anticonvulsant effects exerted by quinazolinone was less efficient than those produced by phenobarbitone. In conclusion, quinazolinone compounds II and IV are more likely to be the most potent as CNS depressant compounds, whereas compound V appears to be the least efficient one. | ||||
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