[Substances with central nervous system activity. Derivatives of octahydro-1,4-dihydroxypyrrolo(1,2-a)pyrazine-6-carboxylic acids].
Compounds with potential activity on the Central Nervous System were prepared starting either from 2,5-diethoxycarbonylpyrrolidine or from N-benzyloxycarbonyl-2,5-pyrrolidinedicarboxylic acid anhydride. By the Arndt-Eistert reaction it was possible to obtain chain lengthening at position 6. The carboxy group was also successfully reduced to a hydroxymethyl group. The synthetic work was completed with the synthesis of some derivatives having a phenyl ring condensed at position 7 and 8. Some pharmacological data on the Central Nervous System depressant activity of the prepared compounds are also reported.
D000374:Aggression / Q000187:drug effects; D000818:Animals; D000927:Anticonvulsants / Q000494:pharmacology; D001522:Behavior, Animal / Q000187:drug effects; D002490:Central Nervous System / Q000187:drug effects*; D055598:Chemical Phenomena; D002621:Chemistry; D006801:Humans; D006993:Hypnotics and Sedatives / Q000494:pharmacology*; D007928:Lethal Dose 50; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D011719:Pyrazines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D011758:Pyrroles / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D051381:Rats
D000927:Anticonvulsants; D006993:Hypnotics and Sedatives; D011719:Pyrazines; D011758:Pyrroles
Sostanze attive sul sistema nervoso centrale. Derivati di acidi ottaidro-1,4-diossopirrolo[1,2-a]pirazino-6-carbossilici.