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Synthesis and anticonvulsant activities of N -Cbz-α-aminoglutarimidooxy carboxylate derivatives

Synthesis and anticonvulsant activities of N -Cbz-α-aminoglutarimidooxy carboxylate derivatives Previous studies on the anticonvulsant activity of N -Cbz-α-aminoglutarimides have shown that the derivatives of N -Cbz-α-amino- N -alkoxy glutarimide have significant anticonvulsant activity. In addition, their anticonvulsant activities are dependent on the presence of N -alkoxy groups. Based on these results, a series of N -Cbz-α-amino-glitarimidooxy carboxylates derivatives ( 3a-e ) were synthesized in moderate yield using a known synthetic procedure. Their anticonvulsant activities were evaluated using the maximal electroshock seizure (MES) test, the pentylene tetrazole induced seizure (PTZ) test, and the strychinine (Str) threshold test with the ultimate aim of developing more active anticonvulsants. None of the compounds ( 3a-e ) tested showed anticonvulsant activity in the MES and PTZ test. However, all the compounds tested exhibited significant anticonvulsant activity in the Str. test. The most active compound in the Str. test was the methyl ester of N -Cbz-α-amino-glutarimidooxy acetic acid 3a (ED 50 =42.9 mg/kg). http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Archives of Pharmacal Research Springer Journals

Synthesis and anticonvulsant activities of N -Cbz-α-aminoglutarimidooxy carboxylate derivatives

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References (5)

Publisher
Springer Journals
Copyright
Copyright © 2006 by The Pharmaceutical Society of Korea
Subject
Pharmacy; Pharmacy; Pharmacology/Toxicology
ISSN
0253-6269
eISSN
1976-3786
DOI
10.1007/BF02969416
Publisher site
See Article on Publisher Site

Abstract

Previous studies on the anticonvulsant activity of N -Cbz-α-aminoglutarimides have shown that the derivatives of N -Cbz-α-amino- N -alkoxy glutarimide have significant anticonvulsant activity. In addition, their anticonvulsant activities are dependent on the presence of N -alkoxy groups. Based on these results, a series of N -Cbz-α-amino-glitarimidooxy carboxylates derivatives ( 3a-e ) were synthesized in moderate yield using a known synthetic procedure. Their anticonvulsant activities were evaluated using the maximal electroshock seizure (MES) test, the pentylene tetrazole induced seizure (PTZ) test, and the strychinine (Str) threshold test with the ultimate aim of developing more active anticonvulsants. None of the compounds ( 3a-e ) tested showed anticonvulsant activity in the MES and PTZ test. However, all the compounds tested exhibited significant anticonvulsant activity in the Str. test. The most active compound in the Str. test was the methyl ester of N -Cbz-α-amino-glutarimidooxy acetic acid 3a (ED 50 =42.9 mg/kg).

Journal

Archives of Pharmacal Research – Springer Journals

Published: Jun 1, 2006

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