Synthesis and anticonvulsant activity of some potential thiazolidinonyl 2-oxo/thiobarbituric acids.
A series of 5-[(N-substituted benzylidenylimino)amino]-2-oxo/thiobarbituric acids (3a-3h) have been synthesized by the condensation of 5-hydrazino-2-oxo/thiobarbituric acids (2a-2b) with various aromatic aldehydes. Cycloaddition of thioglycolic acid to 3a-3h, yielded 5-[(2'-substituted phenyl-4'-oxothiazolidin-3'-yl)amino]-2-oxo/thiobarbituric acids (4a-4h). All these compounds were screened, in vivo, for their anticonvulsant activity and acute toxicity studies. Compounds 4f and 4g were found to be most potent compounds of this series and were compared with the reference drugs, phenytoin sodium, lamotrigine and sodium valproate. The structures of these compounds have been established by IR, 1H NMR and mass spectroscopic data.
Agarwal
A
A
Medicinal Chemistry Division, Department of Pharmacology, LLRM Medical College, Meerut 250004, U.P., India.
Lata
S
S
Saxena
K K
KK
Srivastava
V K
VK
Kumar
A
A
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D001463:Barbiturates / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D003500:Cyclization; D004353:Drug Evaluation, Preclinical; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D051379:Mice; D015394:Molecular Structure; D012640:Seizures / Q000188:drug therapy; D012680:Sensitivity and Specificity; D013237:Stereoisomerism; D053778:Thiazolidines / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity
D000927:Anticonvulsants; D001463:Barbiturates; D053778:Thiazolidines; C516493:thiazolidinonyl 2-oxobarbituric acid; C516494:thiazolidinonyl 2-thiobarbituric acid