Synthesis and anticonvulsant properties of new N-[(4-arylpiperazin-1-yl)-methyl] derivatives of 3-aryl pyrrolidine-2,5-dione and 2-aza-spiro[4.4]nonane-1,3-dione.
A series of N-[(4-arylpiperazin-1-yl)-methyl] derivatives of 3-arylpyrrolidine-2,5-dione and 2-aza-spiro[4.4]nonane-1,3-dione were synthesized and tested for anticonvulsant activity in the maximum electroshock seizure (MES) and metrazole seizure threshold (sc.MET) tests. The most potent in the series were N-[[4-(3-chlorophenyl)-piperazin-1-yl]-methyl]-3-(2-chlorophenyl)-pyrrolidine-2,5-dione (ED50=14.18 mg/kg) and N-[[4-(2-methoxyphenyl)-piperazin-1-yl]-methyl]-3-(3-bromophenyl)-pyrrolidine-2,5-dione (ED50=33.64 mg/kg). Structures of the novel compounds were confirmed by elemental and spectral analyses.
Obniska
Jolanta
J
Department of Medicinal Chemistry, Jagiellonian University Medical College, Medyczna 9, Pl 30-688 Cracow, Poland. mfobnisk@cyf-kr.edu.pl
Zagorska
Agnieszka
A
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000627:therapeutic use; D004597:Electroshock / Q000379:methods; D051379:Mice; D010879:Piperazines / Q000138:chemical synthesis* / Q000627:therapeutic use; D011759:Pyrrolidines / Q000138:chemical synthesis* / Q000627:therapeutic use; D051381:Rats; D012640:Seizures / Q000188:drug therapy
D000927:Anticonvulsants; D010879:Piperazines; D011759:Pyrrolidines