Search for new anticonvulsant compounds. Part 1: Synthesis, physicochemical and anticonvulsant properties of new derivatives of alpha-amino-gamma-phthalimidobutyric acid.

Abstract

Synthesis and physicochemical properties of new derivatives of alpha-substituted gamma-phthalimidobutyric acid are described. N-substituted amides of alpha-(4-phenylpiperazine)-gamma- phthalimidobutyric acid were prepared by condensation of the acid with the corresponding derivatives of benzylamine in the presence of BOP reagent. 2-(4-Phenylpiperazine)- or 2-(4-benzylpiperidine)-4-phthalimidobutyric acid were esterified with alkyl bromide in the presence of DBU or tetrabutylammonium bromide as catalyst. The obtained compounds were evaluated for anticonvulsant activity. 2-(4-Phenylpiperazine)-4-phthalimidobutyric acid and three N-substituted amides of this acid displaced protection against MES and scMet-induced seizures.

• Authors: B Malawska, A Zejc
• Journal: Die Pharmazie (Pharmazie) Vol. 50 Issue 11 Pg. 722-5 (Nov 1995) ISSN: 0031-7144 [Print] Germany
• PMID: 8570669 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Anticonvulsants
• Phthalimides
• Pentylenetetrazole

Topics

• Animals
• Anticonvulsants (chemical synthesis, pharmacology)
• Chemical Phenomena
• Chemistry, Physical
• Electroshock
• Mice
• Pentylenetetrazole
• Phthalimides (chemical synthesis, pharmacology)
• Rats
• Seizures (chemically induced, prevention & control)