Design and synthesis of some new derivatives of 3H-quinazolin-4-one with promising anticonvulsant activity.
作者： Abdel Ghany Aly El-Helby , Mohammed Hemeda Abdeil Wahab
DOI:
关键词: Condensation reaction 、 Chemistry 、 Low dose 、 Phenylisocyanate 、 Stereochemistry 、 Reference drug 、 Quinazolin-4-one 、 Potassium 、 Sodium 、 Anticonvulsant 、 Medicinal chemistry
摘要: A new series of 3-substituted (methyl, ethyl or phenyl)-3H-quinazolin-4-one derivatives (4a-1) were synthesized through condensation reaction their potassium salts (3a-1) with methyl, and phenylisocyanate. The newly evaluated for anticonvulsant activity. It was found that these compounds showed the highest activity at low doses (50-100 mg kg - 1 ), whereas over 100 they a stimulant effect on central nervous system even potentiated convulsive agent, pentylenetetrazole, in mice. halogenated derivatives, 3-methyl, 3-ethyl 3-phenyl-6-mono 6,8-disubstituted-3H-quinazolin-4-one (4m-z) also Reduced recorded. Phenobarbitone sodium used as reference drug.
参考文章(4)
Junichi Tani, Yoshihisa Yamada, Toyonari Oine, Takashi Ochiai, Ryuichi Ishida, Ichizo Inoue, Studies on biologically active halogenated compounds. 1. Synthesis and central nervous system depressant activity of 2-(fluoromethyl)-3-aryl-4(3H)-quinazolinone derivatives. Journal of Medicinal Chemistry. ,vol. 22, pp. 95- 99 ,(1979) , 10.1021/JM00187A021
M. J. Kornet, T. Varia, W. Beaven, Synthesis and anticonvulsant activity of 3‐amino‐4(3H)‐quinazolinones Journal of Heterocyclic Chemistry. ,vol. 20, pp. 1553- 1555 ,(1983) , 10.1002/JHET.5570200623
Margaret M. Endicott, Betty W. Alden, Mary L. Sherrill, Quinazoline derivatives; the synthesis of 4-(3'-diethylaminopropoxy)-6-chloroquinazoline (SN 12,254). Journal of the American Chemical Society. ,vol. 68, pp. 1303- 1304 ,(1946) , 10.1021/JA01211A057
Alvin S. Wheeler, W. M. Oates, THE BROMINATION OF ANTHRANILIC ACID. Journal of the American Chemical Society. ,vol. 32, pp. 770- 773 ,(1910) , 10.1021/JA01924A009