Synthesis and pharmacological screening of some N-carboxymethylbarbituric acid derivatives. I.
Reaction of haloacetate with barbital and methylphenobarbital in polar aprotic solvents in the presence of anhydrous K2CO3 gave N-carboalkoxymethyl derivatives in good yields. Acidic hydrolysis of the latter compounds affords N-carboxymethyl derivatives of barbital 8 or methylphenobarbital 7. From acid 7 and 8 via acid chlorides, amides 11--20 were prepared. These amides lack anticonvulsant activity and show only slight sedative and analgesic action.
D000700:Analgesics; D000818:Animals; D001463:Barbiturates / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D003292:Convulsants; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects
D000700:Analgesics; D001463:Barbiturates; D003292:Convulsants