Substituted quinazolones as potent anticonvulsants and enzyme inhibitors.
A series of 6,8-disubstituted 3-[5- [[2-hydroxy-3-[(substituted phenyl)amino]propyl]thio]-1,3,4-thiadizol-2-yl] 2-methyl-4(3)- quinazolinones were synthesized whose structures were confirmed by elemental analyses, IR, NMR and mass spectral studies. All these compounds were evaluated in vivo for anticonvulsant and analgesic activities and in vitro for monoamine oxidase and succinate dehydrogenase enzyme inhibitory activities using rat brain homogenate as a source of enzyme at final concentration of 1 x 10(-4) mol/l. ALD50 values indicated their relatively nontoxic nature.
Shrimali
M
M
Department of Pharmacology and Therapeutics, King George's Medical College, Lucknow, India.
Kalsi
R
R
Dixit
K S
KS
Barthwal
J P
JP
D000700:Analgesics; D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis*; D001921:Brain / Q000187:drug effects / Q000201:enzymology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis*; D005260:Female; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D008996:Monoamine Oxidase Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D011799:Quinazolines / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D051381:Rats; D013385:Succinate Dehydrogenase / Q000037:antagonists & inhibitors
D000700:Analgesics; D000927:Anticonvulsants; D004791:Enzyme Inhibitors; D008996:Monoamine Oxidase Inhibitors; D011799:Quinazolines; D013385:Succinate Dehydrogenase