SEARCH FOR NEW ANTICONVULSANT COMPOUNDS .1. SYNTHESIS, PHYSICOCHEMICAL AND ANTICONVULSANT PROPERTIES OF NEW DERIVATIVES OF ALPHA-AMINO-GAMMA-PHTHALIMIDOBUTYRIC ACID
B. Malawska et A. Zejc, SEARCH FOR NEW ANTICONVULSANT COMPOUNDS .1. SYNTHESIS, PHYSICOCHEMICAL AND ANTICONVULSANT PROPERTIES OF NEW DERIVATIVES OF ALPHA-AMINO-GAMMA-PHTHALIMIDOBUTYRIC ACID, Die Pharmazie, 50(11), 1995, pp. 722-725
Synthesis and physicochemical properties of new derivatives of alpha-s
ubstituted gamma-phthalimidobutyric acid are described. N-substituted
amides of lpha-(4-phenylpiperazine)-gamma-phthalimidobutyric acid were
prepared by condensation of the acid with the corresponding derivativ
es of benzylamine in the presence of BOP reagent. 2-(4-Phenylpiperazin
e)- or 2- (4-benzylpiperidine)-4-phthalimidobutyric acid were esterifi
ed with alkyl bromide in the presence of DBU or tetrabutylammonium bro
mide as catalyst. The obtained compounds were evaluated for anticonvul
sant activity. 2-(4-Phenylpiperazine)4-phthalimidobutyric acid and thr
ee N-substituted amides of this acid displaced protection against MES
and scMet-induced seizures.